CN1048497C - 4-氰基苯基亚氨基杂环化合物 - Google Patents

4-氰基苯基亚氨基杂环化合物 Download PDF

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CN1048497C
CN1048497C CN94117303A CN94117303A CN1048497C CN 1048497 C CN1048497 C CN 1048497C CN 94117303 A CN94117303 A CN 94117303A CN 94117303 A CN94117303 A CN 94117303A CN 1048497 C CN1048497 C CN 1048497C
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O·沙尔纳
R·安德里
M·W·德鲁斯
M·多林格
H·J·桑特尔
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Abstract

本发明涉及新的通式(Ⅰ)的4-氰基苯基亚氨基杂环化合物，它们的制备方法，它们作为除草剂的用途，以及用于它们合成的新的中间体，其中各取代基的定义如说明书所述。

Description

4-氰基苯基亚氨基杂环化合物
本发明涉及新的4-氰基苯基亚氨基杂环化合物、它们的制备方法、它们作为除草剂的用途、以及用于它们合成的新的中间体。
已知某些卤代芳基亚氨基杂环化合物表现出除草性质(参见EP-A 238711、EP-A 273417、EP-A 312064、EP-A 410265、EP-A457714、WO-A 92/21684)。然而，这些已知化合物的除草活性以及它们可被栽培植物耐受的能力未必令人完全满意。
现已发现新的通式(I)4-氰基苯基亚氨基杂环化合物：其中：
R1代表氢或卤素，
R2代表卤素、氰基、羟基、氨基、或下列基团之一：-X-R3、-N(R4)-CO-R5或-N(R4)-SO2R5，其中：
X代表氧、硫或单键，
R3代表可各自被任意取代的烷基、链烯基、炔基环烷基环烷基烷基、芳基、芳基烷基、杂环基或杂环基烷基。
R4代表氢或烷基，及
R5代表可各自被任意取代的烷基、链烯基、炔基  环烷基、环烷基烷基、芳基或芳基烷基，
A代表可各自被任意取代的链烷二基或链烯二基，
E代表氮或碳，和
G代表氮或代表碳，所述原子通过外单键与氢或烷基键连，或通过外双键与氧或硫键连，
其中，当E代表氮时，A不代表任意取代的1，3-亚丙基。
新的通式(I)4-氰基苯基亚氨基杂环化合物由下列方法制得：
a).使通式(II)的取代的硫代羰基氨基化合物：
Figure C9411730300081
其中A、R1和R2具有上述定义，与氧化剂或脱氢剂任选在反应辅助剂存在下以及任选在稀释剂存在下反应，或
b).使通式(III)的取代的硫代羰基氨基化合物：
其中A、R1和R2具有上述定义，与光气任选在稀释剂存在下反应，或
c).使通式(Ia)的4-氰基苯基亚氨基杂环化合物：
Figure C9411730300092
其中：R1、A、E和G具有上述定义，和
      X1代表卤素，
与通式(IV)或(V)的亲核化合物：
H-X-R3             (IV)       H-N(R4)-SO2R5            (V)
其中：X、R3、R4和R5具有上述定义，或与这些化合物的碱金属盐类任选在酸性接受体存在下以及任选在稀释剂存在下反应。
按照下式路线，使通式(VI)的亚氨基杂环化合物与通式(VII)的4-卤代苄腈类反应也可制得新的式(I)化合物(R1、R2、A、E和G定义如上，X2：卤素)：
Figure C9411730300101
新的通式(I)的4-氰基苯基亚氨基杂环化合物以强的和选择性的除草活性而著称。
在上述定义中，饱和或不饱和烃链如烷基、链烷二基、链烯基、链烯二基成炔基在各种情况下可是直链或支链。
卤素通常代表氟、氯、溴或碘，优选代表氟、氯或溴，特别的是代表氟或氯。
本发明优选涉及式(I)化合物，其中：
R1代表氢、氟、氯或溴，
R2代表氟、氯、溴、氰基、羟基、氨基或下列基团之一：-X-R3、-N(R4)-CO-R5或-N(R4)-SO2R5，其中：
X代表氧、硫或单键，
R3代表具有1-8个碳原子的烷基，所述烷基可被氟、氯、溴、氰基、羧基、C1-C4烷氧基、C1-C4烷氧基-C1-C4烷氧基、C1-C4烷硫基、C1-C4烷基羰基、C1-C4烷氧羰基或C5-C6环烷氧基羰基任意取代，
R3另外代表各自具有2-8个碳原子的链烯基或炔基，并且它们可各自被氟、氯或溴任意取代，
R3另外代表各自在环烷基部分具有3-8个碳原子并且在烷基部分任选具有1-4个碳原子的环烷基或环烷基烷基，并且它们可各自被氟、氯、溴、氰基、羧基、C1-C4烷基或C1-C4烷氧基羰基任意取代，或代表可各自被任意取代的苯基、苄基、苯乙基、苯丙基或苯丁基，或代表各自具有3-8个环原子(其中至少一个是氧、硫或氮原子且任选1-3个环原子是另外的氮原子)的各自任选被取代的杂环基、杂环基甲基、杂环基乙基、杂环基丙基或杂环基丁基，其中杂环基可是饱和或不饱和的，且上述环基任选含有下列取代基：卤素、氰基、硝基、羧基、氨基甲酰基、C1-C4烷基、C1-C4卤代烷基、C1-C4烷氧基、C1-C4卤代烷氧基、C1-C4烷硫基、C1-C4卤代烷硫基、C1-C4烷基亚磺酰基、C1-C4卤代烷基亚磺酰基、C1-C4烷基磺酰基、C1-C4卤代烷基磺酰基和C1-C4烷氧羰基，
R4代表氢或代表具有1-8个碳原子的烷基，及
R5代表具有1-8个碳原子的烷基，且所述烷基可被氟、氯、溴、氰基、羧基、C1-C4烷氧基、C1-C4烷氧基-C1-C4烷氧基、C1-C4烷硫基、C1-C4烷基羰基或C1-C4烷氧羰基任意取代，
R5另外代表各自具有2-8个碳原子的链烯基或炔基，且所述基团可各自被氟、氯或溴任意取代，
R5另外代表各自在环烷基部分具有3-8个碳原子并且在烷基部分任选具有1-4个碳原子的环烷基或环烷基烷基，并且所述基团可各自被氟、氯、溴、氰基、羧基、C1-C4烷基或C1-C4烷氧羰基任意取代，或代表在芳基部分具有6或10个碳原子且在烷基部分任选具有1-4个碳原子的芳基或芳烷基，并且所述基团各自可被下列基团任意取代：氟、氯、溴、氰基、硝基、羧基、氨基甲酰基：C1-C4烷基、C1-C4烷氧基、C1-C4烷硫基、C1-C4烷基亚磺酰基或C1-C4烷基磺酰基(它们各自可被氟和/或氯任意取代)；二甲基氨基磺酰基或二乙基氨基磺酰基；C1-C4烷氧羰基(它可被氟、氯、溴、甲氧基或乙氧基任意取代)；苯基、苯基甲基、苯氧基、苯硫基、苯基亚磺酰基或苯基磺酰基(它们各自可被氟、氯、溴、氰基、甲基、甲氧基、三氟甲基、二氟甲氧基和/或三氟甲氧基任意取代)，
A代表各自具有2-6个碳原子的链烷二基或链烯二基，且所述基团可各自被氟、氯、溴或C1-C4烷基(它可被氟和/或氯任意取代)任意取代，
E代表氮或碳，和
G代表氮或碳，所述原子通过外单键与氢或C1-C6烷基键连，或通过外双键与氧或硫键连，
其中当E代表氮时，A不代表任意取代的1，3-亚丙基。
本发明特别涉及式(I)化合物，其中：
R1代表氢、氟或氯，
R2代表氟、氯、溴、氰基、羟基、氨基、或下列基团之一：-X-R3、-N(R4)-CO-R5或-N(R4)-SO2R5，其中：
X代表氧、硫或单键，
R3代表甲基、乙基、正丙基或异丙基、正丁基、异丁基、仲丁基或叔丁基，它们可各自被下列基团任意取代：氟、氯、溴、氰基、羧基、甲氧基、乙氧基、甲氧基乙氧基、乙氧基乙氧基、甲硫基、乙硫基、乙酰基、丙酰基、甲氧羰基或乙氧羰基，
R3另外代表可各自被氟或氯任意取代的烯丙基、丁烯基、1-甲基烯丙基、炔丙基或1-甲基炔丙基，
R3另外代表环丙基、环丁基、环戊基、环己基、环丙基甲基、环丁基甲基、环戊基甲基或环己基甲基，它们可各自被氟、氯、甲基、乙基、正丙基、异丙基、甲氧羰基或乙氧羰基任意取代，
R4代表氢、甲基、乙基、正丙基、异丙基、正丁基、异丁基或仲丁基，
R5代表甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基，它们可各自被下列基团任意取代：氟、氯、溴、氰基、羧基、甲氧基、乙氧基、甲氧基乙氧基、乙氧基乙氧基、甲硫基、乙硫基、乙酰基、丙酰基、甲氧羰基或乙氧羰基，
R5另外代表可各自被氟或氯任意取代的烯丙基、丁烯基、1-甲基烯丙基、炔丙基或1-甲基炔丙基，
R5另外代表环丙基、环丁基、环戊基、环己基、环丙基甲基、环丁基甲基、环戊基甲基或环己基甲基，它们可各自被氟、氯、甲基、乙基、正丙基或异丙基任意取代，
R5另外代表苯基、萘基、苄基或苯乙基，它们可各自被下列基团任意取代：氟、氯、溴、氰基、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基、叔丁基、甲氧基、乙氧基、甲硫基、乙硫基、甲基亚磺酰基、乙基亚磺酰基、甲基磺酰基、乙基磺酰基、三氟甲基、二氟甲氧基、三氟甲氧基、三氟甲硫基、三氟甲基亚磺酰基、三氟甲基磺酰基、二甲基氨基磺酰基、甲氧羰基、乙氧羰基、苯基、苯氧基或苯基磺酰基，
A代表丙烷-1，3-二基(1，3-亚丙基)、丁烷-1，4-二基(1，4-亚丁基)、1-丙烯-1，3-二基、1-丁烯-1，4-二基或2-丁烯-1，4-二基，它们可各自被氟、氯、溴、甲基、乙基、正丙基或异丙基任意取代，
E代表氮或碳，和
G代表氨或碳，所述原子通过外单键与氢、甲基、乙基、正丙基、异丙基、正丁基、异丁基、仲丁基或叔丁基键连，或通过外双键与氧键连，
其中，当E代表氮时，A不代表任意被取代的1，3-亚丙基。
特别优选的式(I)化合物是通式(IA)化合物：
Figure C9411730300141
其中：R1、R2和A具有上面特别优选化合物中所述的定义。
另外特别优选的式(I)化合物是通式(IB)化合物：
Figure C9411730300151
其中：R1、R2和A具有上面特别优选化合物中所述的定义。
本发明式(I)化合物的实例列于下表1中：
Figure C9411730300152
表1：式(1)化合物的实例
R1         R2                                    A             E      G
F           O-CH(CH2F)2                         -(CH2)4-    N      CO
F           O-CH2-C(CH3)＝CH2                  -(CH2)4-    N      CO
F                                   -(CH2)4-    N      CO
F           
Figure C9411730300162
                       -(CH2)4-    N      CO
F                                      -(CH2)4-    N      CO
F           
Figure C9411730300164
                       -(CH2)4-    N      CO
F           
Figure C9411730300165
                          -(CH2)4-    N      CO
F           
Figure C9411730300166
                    -(CH2)4-    N      CO表1(续)
R1           R2                        A               E       G
F             S-CH2-COOC5H11-n        -(CH2)4-     N       CO
F       
Figure C9411730300171
            -(CH2)4-     N       CO
F                         -(CH2)4-      N       CO
F             O-CH2CH2-OCH(CH2F)2  -(CH2)4-      N       CO
F             S-CH(CH3)2             -(CH2)4-      N       CO
F             O-CH2-CCl＝CH2         -(CH2)4-      N       CO
F             
Figure C9411730300173
            -(CH2)4-      N       CO表1(续)
R1      R2                              A               E       G
F        O-CH2CN                         -(CH2)4-      N      CO
F        O-CH2COOC2H4-OCH3           -(CH2)4-      N      CO
F        O-CH2-COO-CH(CH3)COOC2H5    -(CH2)4-      N      CO
F        OCH2-COOCH2-COOC2H5         -(CH2)4-      N      CO
F        O-CHF2                          -(CH2)4-      N      CO
F        O-CH2CH2-OCH2CF3            -(CH2)4-      N      CO
F        OCH2CF3                        -(CH2)4-      N      CO
F        OCF3                            -(CH2)4-      N      CO
F        OCH2CH(CH3)-OC2H5           -(CH2)4-      N      CO
F                            -(CH2)4-       N      CO
F        OCH2-CH＝CH2                  -(CH2)4-      N      CO
F        OH                               -(CH2)4-      N      CO
F        OCH2-C≡CH                     -(CH2)4-       N      CO表1(续)
R1      R2                        A               E      G
F        SCH2C≡CH                 -(CH2)4-      N      CO
F        OCH2COOC2H5            -(CH2)4-      N      CO
F        S-C(CH3)3               -(CH2)4-      N      CO
F        OCH2-COOC5H11-n        -(CH2)4-      N      CO
F        OCH(CH3)-COOC2H5       -(CH2)4-      N      CO
F        OCH2CH2-OCH3           -(CH2)4-      N      CO
F        OCH2CH2-OC2H5         -(CH2)4-      N      CO
F        O(CH2CH2O)2-C2H5     -(CH2)4-      N      CO
F        S-C3H7-n                 -(CH2)4-      N      CO表1(续)
R1        R2                       A               E      G
F          S-C2H5                  -(CH2)4-     N      CO
F          S-CH3                    -(CH2)4-      N      CO
F          S-CH2COOC2H5           -(CH2)4-     N      CO
F          SCH2CH2-COOC2H5      -(CH2)4-      N      CO
F          O-CH2-C≡C-CH3          -(CH2)4-      N      CO
F          OCH2-CH＝CH-Cl           -(CH2)4-      N      CO
F          O-CH(CH3)C≡CH           -(CH2)4-      N      CO
F          OCH(CH3)C≡C-CH3        -(CH2)4-      N      CO
F          O-CH(CH3)CH＝CH2        -(CH2)4-      N      CO
F          OCH2CH＝CH-CH3          -(CH2)4-      N      CO
F          O-CH3                    -(CH2)4-      N      CO
F          O-C2H5                  -(CH2)4-      N      CO
F          O-C3H7-n                -(CH2)4-      N      CO
F          O-C3H7-iso              -(CH2)4-      N      CO
F          
Figure C9411730300201
              -(CH2)4-      N      CO表1(续)
R1          R2                    A               E      G
F                         -(CH2)4-     N      CO
F            NHCH3                -(CH2)4-      N      CO
F            NHC2H5              -(CH2)4-      N      CO
F            N(CH3)2             -(CH2)4-      N      CO
F            NH-CH2-COOC2H5     -(CH2)4-      N      CO
F                            -(CH2)4-      N      CO
F            
Figure C9411730300213
              -(CH2)4-      N      CO
F            NH-SO2CH3           -(CH2)4-      N      CO
F            NH-SO2C2H5         -(CH2)4-      N      CO表1(续)
R1       R2                         A               E      G
F         NH-SO2C3H7-n           -(CH2)4-      N      CO
F         NH-SO2C3H7-i           -(CH2)4-      N      CO
F         NH-SO2C4H9-n           -(CH2)4-      N      CO
F         NH-SO2C8H17-n          -(CH2)4-      N      CO
F         NH-COCH3                 -(CH2)4-      N      CO
F         NH-COC2H5               -(CH2)4-      N      CO
F         NH-COCF3                 -(CH2)4-      N      CO
F         N(CH3)-SO2CH3         -(CH2)4-      N      CO
F         N(CH3)-SO2C2H5       -(CH2)4-      N      CO
F         N(CH3)-SO2C3H7-n     -(CH2)4-      N      CO
F         NH-SO2CF3              -(CH2)4-      N      CO
F                       -(CH2)4-      N      CO表1(续)
R1        R2                      A               E      G
F          NH-SO2-C4F9-n        -(CH2)4-      N      CO
F          N(CH3)SO2CF3         -(CH2)4-      N      CO
F       
Figure C9411730300231
         -(CH2)4-      N      CO
F       
Figure C9411730300232
       -(CH2)4-      N      CO
F        
Figure C9411730300233
    -(CH2)4-      N      CO
H          OCH2CF3                -(CH2)4-      N      CO
H          OCF3                    -(CH2)4-      N      CO
H          OCH2CH(CH3)-OC2H5   -(CH2)4-      N      CO
H                       -(CH2)4-      N      CO表1(续)
R1      R2                        A               E      G
H        OCH2-CH＝CH2             -(CH2)4-      N      CO
H        OH                         -(CH2)4-      N      CO
H        OCH2-C≡CH                -(CH2)4-      N      CO
H        SCH2C≡CH                 -(CH2)4-      N      CO
H        OCH2COOC2H5             -(CH2)4-      N      CO
H        S-C(CH3)3                -(CH2)4-      N      CO
H        OCH2-COOC5H11-n         -(CH2)4-      N      CO
H        OCH(CH3)-COOC2H5        -(CH2)4-      N      CO
H        OCH2CH2-OCH3            -(CH2)4-      N      CO
H        OCH2CH2-OC2H5          -(CH2)4-      N      CO
H        O(CH2CH2O)2-OC2H5    -(CH2)4-      N      CO
H        S-C3H7-n                 -(CH2)4-      N      CO表1(续)
R1      R2                      A               E      G
H        S-C2H5                 -(CH2)4-      N      CO
H        S-CH3                   -(CH2)4-      N      CO
H        S-CH2COOC2H5          -(CH2)4-     N      CO
H        SCH2CH2-COOC2H5     -(CH2)4-      N      CO
H        O-CH2-C≡CH3           -(CH2)4-      N      CO
H        OCH2-CH＝CH-Cl          -(CH2)4-      N      CO
H        O-CH(CH3)C≡CH          -(CH2)4-      N      CO
H        OCH(CH3)C≡C-CH3       -(CH2)4-      N      CO
H        O-CH(CH3)CH＝CH2       -(CH2)4-      N      CO
H        OCH2CH＝CH-CH3         -(CH2)4-      N      CO表1(续)
R1      R2                     A               E      G
H        O-CH3                  -(CH2)4-      N      CO
H        O-C2H5                -(CH2)4-      N      CO
H        O-C3H7-n              -(CH2)4-      N      CO
H        O-C3H7-iso            -(CH2)4-      N      CO
H        
Figure C9411730300261
           -(CH2)4-      N      CO
H        
Figure C9411730300262
              -(CH2)4-      N      CO
H        O-CH(CH2F)2           -(CH2)4-      N      CO
H        O-CH2-C(CH3)＝H2     -(CH2)4-      N      CO
H        
Figure C9411730300263
            -(CH2)4-      N      CO
H                   -(CH2)4-      N      CO
H        
Figure C9411730300265
            -(CH2)4-      N      CO表1(续)
R1      R2                             A            E    G
H        
Figure C9411730300271
                   -(CH2)4-    N    CO
H        
Figure C9411730300272
                -(CH2)4-    N    CO
H        
Figure C9411730300273
            -(CH2)4-    N    CO
H        S-CH2-COOC5H11-n           -(CH2)4-    N    CO
H        
Figure C9411730300274
                -(CH2)4-    N    CO
H        
Figure C9411730300275
                -(CH2)4-    N    CO
H        O-CH2CH2-O)CH(CH2F)2     -(CH2)4-    N    CO
H        S-CH(CH3)2                  -(CH2)4-    N    CO表1(续)
R1      R2                             A             E    G
H        O-CH2-CCl＝CH2               -(CH2)4-    N    CO
H        
Figure C9411730300281
                    -(CH2)4-    N    CO
H        O-CH2CN                       -(CH2)4-    N    CO
H        O-CH2COOC2H4-OCH3         -(CH2)4-    N    CO
H        O-CH2-COO-CH(CH3)COOC2H5  -(CH2)4-    N    CO
H        OCH2-COOCH2-COOC2H5       -(CH2)4-    N    CO
H        O-CHF2                        -(CH2)4-    N    CO
H        O-CH2CH2-OCH2CF3          -(CH2)4-    N    CO
H        NHCH3                         -(CH2)4-    N    CO
H        NHC2H5                       -(CH2)4-    N    CO
H        N(CH3)2                      -(CH2)4-    N    CO
H        NH-CH2-COOC2H5              -(CH2)4-    N    CO表1(续)
R1       R2                         A             E    G
H                              -(CH2)4-    N    CO
H         
Figure C9411730300292
               -(CH2)4-    N    CO
H         NH-SO2CH3                 -(CH2)4-    N    CO
H         NH-SO2C2H5               -(CH2)4-    N    CO
H         NH-SO2C3H7-n             -(CH2)4-    N    CO
H         NH-SO2C3H7-i             -(CH2)4-    N    CO
H         NH-SO2C4H9-n             -(CH2)4-    N    CO
H         NH-SO2C8H17-n            -(CH2)4-    N    CO
H         NH-COCH3                   -(CH2)4-    N    CO
H         NH-COC2H5                 -(CH2)4-    N    CO表1(续)
R1        R2                         A             E    G
H          NH-COCF3                   -(CH2)4-    N    CO
H          N(CH3)-SO2CH3           -(CH2)4-    N    CO
H          N(CH3)-SO2C2H5         -(CH2)4-    N    CO
H          N(CH3)-SO2C3H7-n       -(CH2)4-    N    CO
H          NH-SO2CF3                -(CH2)4-    N    CO
H          
Figure C9411730300301
               -(CH2)4-    N    CO
H          NH-SO2-C4F9-n           -(CH2)4-    N    CO
H          N(CH3)SO2CF3            -(CH2)4-    N    CO
H                       -(CH2)4-    N    CO
H          
Figure C9411730300303
         -(CH2)4-    N    CO表1(续)
R1         R2                          A             E    G
H           
Figure C9411730300311
   -(CH2)4-    N    CO
Cl          OCH2CF3                   -(CH2)4-    N    CO
Cl          OCF3                       -(CH2)4-    N    CO
Cl          OCH2CH(CH3)-OC2H5      -(CH2)4-    N    CO
Cl          
Figure C9411730300312
              -(CH2)4-    N    CO
Cl          OCH2-CH＝CH2             -(CH2)4-    N    CO
Cl          OH                         -(CH2)4-    N    CO
Cl          OCH2-C≡CH                -(CH2)4-    N    CO
Cl          SCH2C≡CH                 -(CH2)4-    N    CO
Cl          OCH2COOC2H5            -(CH2)4-    N    CO
Cl          S-C(CH3)3               -(CH2)4-    N    CO表1(续)
R1           R2                            A             E    G
Cl            OCH2-COOC5H11-n            -(CH2)4-    N    CO
Cl            OCH(CH3)-COOC2H5           -(CH2)4-    N    CO
Cl            OCH2CH2-OCH3               -(CH2)4-    N    CO
Cl            OCH2CH2-OC2H5             -(CH2)4-    N    CO
Cl            O(CH2CH2O)2-OC2H5        -(CH2)4-    N    CO
Cl            S-C3H7-n                     -(CH2)4-    N    CO
Cl            S-C2H5                       -(CH2)4-    N    CO
Cl            S-CH3                         -(CH2)4-    N    CO
Cl            S-CH2COOC2H5               -(CH2)4-    N    CO
Cl            SCH2CH2-COOC2H5           -(CH2)4-    N    CO
Cl            O-CH2-C≡C-CH3               -(CH2)4-    N    CO
Cl            OCH2-CH＝CH-Cl                -(CH2)4-    N    CO
Cl            O-CH(CH3)C≡CH                -(CH2)4-    N    CO
Cl            OCH(CH3)C≡C-CH3             -(CH2)4-    N    CO
Cl            O-CH(CH3)CH＝CH2             -(CH2)4-    N    CO表1(续)
R1        R2                        A             E     G
Cl         OCH2CH＝CH-CH3           -(CH2)4-    N    CO
Cl         O-CH3                     -(CH2)4-    N    CO
Cl         OC2H5                    -(CH2)4-    N    CO
Cl         O-C3H7-n                 -(CH2)4-    N    CO
Cl         O-C3H7-iso               -(CH2)4-    N    CO
Cl         
Figure C9411730300331
                -(CH2)4-    N    CO
Cl         
Figure C9411730300332
                 -(CH2)4-    N    CO
Cl         O-H(CH2F)2               -(CH2)4-    N    CO
Cl         O-CH2-C(CH3)＝CH2       -(CH2)4-    N    CO
Cl         
Figure C9411730300333
               -(CH2)4-    N    CO
Cl         
Figure C9411730300334
           -(CH2)4-    N    CO
Cl                          -(CH2)4-    N    CO表1(续)
R1          R2                            A             E    G
Cl           
Figure C9411730300341
              -(CH2)4-     N    CO
Cl           
Figure C9411730300342
              -(CH2)4-     N    CO
Cl           
Figure C9411730300343
            -(CH2)4-     N    CO
Cl        S-CH2-COOC5H11-n              -(CH2)4-     N    CO
Cl           
Figure C9411730300344
             -(CH2)4-     N    CO
Cl           
Figure C9411730300345
               -(CH2)4-     N    CO
Cl        O-CH2CH2-OCH(CH2F)2         -C(CH2)4-    N    CO
Cl        S-CH(CH3)2                     -C(CH2)4-    N    CO表1(续)
R1        R2                           A             E    G
Cl         O-CH2-CCl＝CH2              -(CH2)4-    N    CO
Cl         
Figure C9411730300351
                   -(CH2)4-    N    CO
Cl         O-CHCN                         -(CH2)4-    N    CO
Cl         O-CH2COOC2H4-OCH3         -(CH2)4-    N    CO
Cl         O-CH2-COO-CH(CH3)COOC2H5  -(CH2)4-    N    CO
Cl         OCH2-COOCH2-COOC2H5       -(CH2)4-    N    CO
Cl         O-CHF2                        -(CH2)4-    N    CO
Cl         O-CH2CH2-OCH2CF3          -(CH2)4-    N    CO
Cl         NHCH3                         -(CH2)4-    N    CO
Cl         NHC2H5                       -(CH2)4-    N    CO
Cl         N(CH3)2                      -(CH2)4-    N    CO表1(续)
R1        R2                        A             E    G
Cl         NH-CH2COOC2H5          -(CH2)4-    N    CO
Cl         
Figure C9411730300361
               -(CH2)4-    N    CO
Cl         
Figure C9411730300362
                  -(CH2)4-    N    CO
Cl         NH-SO2CH3               -(CH2)4-    N    CO
Cl         NH-SO2C2H5             -(CH2)4-    N    CO
Cl         NH-SO2C3H7-n           -(CH2)4-    N    CO
Cl         NH-SO2C3H7-i           -(CH2)4-    N    CO
Cl         NH-SO2C4H9-n           -(CH2)4-    N    CO
Cl         NH-SO2C8H17-n          -(CH2)4-    N    CO
Cl         NH-COCH3                 -(CH2)4-    N    CO
Cl         NH-COC2H5               -(CH2)4-    N    CO表1(续)
R1           R2                       A             E    G
Cl            NH-COCF3                 -(CH2)4-    N    CO
Cl            N(CH3)-SO2CH3         -(CH2)4-    N    CO
Cl            N(CH3)-SO2C2H5       -(CH2)4-    N    CO
Cl            N(CH3)SO2C3H7-n      -(CH2)4-    N    CO
Cl            NH-SO2CF3              -(CH2)4-    N    CO
Cl            
Figure C9411730300371
            -(CH2)4-    N    CO
Cl            NH-SO2-C4F9-n         -(CH2)4-    N    CO
Cl            N(CH3)SO2CF3          -(CH2)4-    N    CO
Cl            
Figure C9411730300372
        -(CH2)4-    N    CO
Cl            
Figure C9411730300373
     -(CH2)4-    N    CO表1(续)
R1      R2                          A             E    G
Cl       
Figure C9411730300381
    -(CH2)4-    N    CO
F        O-CH(C2F)2                -(CH2)4-    N    CO
F        O-CH2-C(CH3)＝CH2       -(CH2)4-    N    CO
F        
Figure C9411730300382
            -(CH2)4-    N    CO
F        
Figure C9411730300383
             -(CH2)4-    N    CO
F        
Figure C9411730300384
               -(CH2)4-    N    CO
F        
Figure C9411730300385
              -(CH2)4-    N    CO
F                       -(CH2)4-    N    CO表1(续)
R1      R2                         A               E    G
F                   -(CH2)4-      N    CO
F        S-CH2-COOC5H11-n       -(CH2)4-      N    CO
F        
Figure C9411730300392
            -(CH2)4-      N    CO
F        
Figure C9411730300393
            -(CH2)4-      N    CO
F        O-CH2CH2-OCH(CH2F)2   -(CH2)4-      N    CO
F        S-CH(CH3)2              -(CH2)4-      N    CO
F        O-CH2-CCl＝CH2          -(CH2)4-      N    CO
F        
Figure C9411730300394
               -(CH2)4-      N    CO表1(续)
R1      R2                             A                     E    G
F        O-CH2CN                        -(CH2)4-            N    CO
F        O-CH2COOC2H4-OCH3          -(CH2)4-            N    CO
F        O-CH2-COO-CH(CH3)COOC2H5   -(CH2)4-            N    CO
F        OCH2-COOCH2-COOC2H5        -(CH2)4-            N    CO
F        O-CHF2                         -(CH2)4-            N    CO
F        O-CH2CH2-OCH2CF3           -(CH2)4-            N    CO
F        O-CH(CH2F)2                  -CH2-CH＝CH-CH2-     N    CO
F        O-CH2-C(CH3)＝CH2           -CH2-CH＝CH-CH2-     N    CO
F        
Figure C9411730300401
               -CH2-CH＝CH-CH2-     N    CO
F                          -CH2-CH＝CH-CH2-     N    CO表1(续)
R1      R2                         A                    E    G
F        
Figure C9411730300411
                -CH2-CH＝CH-CH2-   N    CO
F        
Figure C9411730300412
              -CH2-CH＝CH-CH2-   N    CO
F                     -CH2-CH＝CH-CH2-    N    CO
F        
Figure C9411730300414
           -CH2-CH＝CH-CH2-    N    CO
F        S-CH2-COOC5H11-n        -CH2-CH＝CH-CH2-    N    CO
F        
Figure C9411730300415
             -CH2-CH＝CH-CH2-    N    CO
F                   -CH2-CH＝CH-CH2-    N    CO
F        O-CH2CH2-OCH(CH2F)2   -CH2-CH＝CH-CH2-     N    CO表1(续)
R1        R2                          A                    E  G
F          S-CH(CH3)2                 -CH2-CH＝CH-CH2-  N  CO
F          O-CH2-CCl＝CH2             -CH2-CH＝CH-CH2-  N  CO
F          
Figure C9411730300421
                   -CH2-CH＝CH-CH2-  N  CO
F          O-CH2CN                      -CH2-CH＝CH-CH2-  N  CO
F          O-CH2COOC2H4-OCH3        -CH2-CH＝CH-CH2-  N  CO
F          O-CH2-COO-CH(CH3)COOC2H5 -CH2-CH＝CH-CH2-  N  CO
F          OCH2-COOCH2-COOC2H5      -CH2-CH＝CH-CH2-  N  CO
F          O-CHF2                       -CH2-CH＝CH-CH2-  N  CO
F          O-CH2CH2-OCH2CF3         -CH2-CH＝CH-CH2-  N  CO
F          OCH2CF3                     -CH2-CH＝CH-CH2-  N  CO
F          OCF3                         -CH2-CH＝CH-CH2-  N  CO表1(续)
R1      R2                     A                    E    G
F        OCH2CH(CH3)-OC2H5 -CH2-CH＝CH-CH2-    N    CO
F        
Figure C9411730300431
           -CH2-CH＝CH-CH2-    N    CO
F        OCH2-CH＝CH2         -CH2-CH＝CH-CH2-    N    CO
F        OH                     -CH2-CH＝CH-CH2-    N    CO
F        OCH2-C≡CH            -CH2-CH＝CH-CH2-    N    CO
F        SCH2C≡CH             -CH2-CH＝CH-CH2-    N    CO
F        OCH2COOC2H5         -CH2-CH＝CH-CH2-    N    CO
F        S-C(CH3)3            -CH2-CH＝CH-CH2-    N    CO
F        OCH2-COOC5H11-n     -CH2-CH＝CH-CH2-    N    CO
F        OCH(CH3)-COOC2H5    -CH2-CH＝CH-CH2-    N    CO
F        OCH2CH2-OCH3        -CH2-CH＝CH-CH2-    N    CO
F        OCH2CH2-OC2H5      -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                         A                      E    G
F         O(CH2CH2O)2-OC2H5     -CH2-CH＝CH-CH2-    N    CO
F         S-C3H7-n                  -CH2-CH＝CH-CH2-    N    CO
F         S-C2H5                    -CH2-CH＝CH-CH2-    N    CO
F         S-CH3                      -CH2-CH＝CH-CH2-    N    CO
F         S-CH2COOC2H5            -CH2-CH＝CH-CH2-    N    CO
F         SCH2CH2-COOC2H5        -CH2-CH＝CH-CH2-    N    CO
F         OCH2-C≡C-CH3             -CH2-CH＝CH-CH2-    N    CO
F         OCH2-CH＝CH-Cl             -CH2-CH＝CH-CH2-    N    CO
F         O-CH(CH3)C＝CH             -CH2-CH＝CH-CH2-    N    CO
F         OCH(CH3)C≡C-CH3          -CH2-CH＝CH-CH2-    N    CO
F         O-CH(CH3)CH＝CH2          -CH2-CH＝CH-CH2-    N    CO
F         OCH2CH＝CH-CH3            -CH2-CH＝CH-CH2-    N    CO
F         O-CH3                      -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                 A                     E    G
F        O-C2H5            -CH2-CH＝CH-CH2-    N    CO
F        O-C3H7-n          -CH2-CH＝CH-CH2-    N    CO
F        O-C3H7-iso        -CH2-CH＝CH-CH2-    N    CO
F        
Figure C9411730300451
         -CH2-CH＝CH-CH2-    N    CO
F        
Figure C9411730300452
          -CH2-CH＝CH-CH2-    N    CO
F        NHCH3              -CH2-CH＝CH-CH2-    N    CO
F        NHC2H5            -CH2-CH＝CH-CH2-    N    CO
F        N(CH3)2           -CH2-CH＝CH-CH2-    N    CO
F        NH-CH2-COOC2H5   -CH2-CH＝CH-CH2-    N    CO
F                      -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                     A                     E    G
F        
Figure C9411730300461
                -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2CH3            -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2C2H5          -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2C3H7-n        -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2C3H7-i        -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2C4H9-n        -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2C8H17-n       -CH2-CH＝CH-CH2-    N    CO
F        NH-COCH3               -CH2-CH＝CH-CH2-    N    CO
F        NH-COC2H5             -CH2-CH＝CH-CH2-    N    CO
F        NH-COCF3               -CH2-CH＝CH-CH2-    N    CO
F        N(CH3)-SO2CH3       -CH2-CH＝CH-CH2-    N    CO
F        N(CH3)-SO2C2H5     -CH2-CH＝CH-CH2-    N    CO
F        N(CH3)-SO2C3H7-n   -CH2-CH＝CH-CH2-    N    CO
F        NH-SO2CF3            -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                       A                       E      G
F        
Figure C9411730300471
          -CH2-CH＝CH-CH2-      N      CO
F        NH-SO2-C4F9-n          -CH2-CH＝CH-CH2-      N      CO
F        N(CH3)SO2CF3           -CH2-CH＝CH-CH2-      N      CO
F        
Figure C9411730300472
           -CH2-CH＝CH-CH2-      N      CO
F        
Figure C9411730300473
        -CH2-CH＝CH-CH2-      N      CO
F             -CH2-CH＝CH-CH2-      N      CO
H        OCH2CF3                 -CH2-CH＝CH-CH2-      N      CO
H        OCF3                     -CH2-CH＝CH-CH2-      N      CO表1(续)
R1      R2                    A                     E    G
H        OCH2CH(CH3)-OC2H5 -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300481
        -CH2-CH＝CH-CH2-    N    CO
H        OCH2-CH＝CH2         -CH2-CH＝CH-CH2-    N    CO
H        OH                     -CH2-CH＝CH-CH2-    N    CO
H        OCH2-C≡CH            -CH2-CH＝CH-CH2-    N    CO
H        SCH2C≡CH             -CH2-CH＝CH-CH2-    N    CO
H        OCH2COOC2H5         -CH2-CH＝CH-CH2-    N    CO
H        S-C(CH3)3            -CH2-CH＝CH-CH2-    N    CO
H        OCH2-COOC5H11-n     -CH2-CH＝CH-CH2-    N    CO
H        OCH(CH3)-COOC2H5    -CH2-CH＝CH-CH2-    N    CO
H        OCH2CH2-OCH3        -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                        A                     E    G
H        OCH2CH2-OC2H5         -CH2-CH＝CH-CH2-    N    CO
H        O(CH2CH2O)2-OC2H5    -CH2-CH＝CH-CH2-    N    CO
H        S-C3H7-n                 -CH2-CH＝CH-CH2-    N    CO
H        S-C2H5                   -CH2-CH＝CH-CH2-    N    CO
H        S-CH3                     -CH2-CH＝CH-CH2-    N    CO
H        S-CH2COOC2H5           -CH2-CH＝CH-CH2-    N    CO
H        SCH2C2-COOC2H5        -CH2-CH＝CH-CH2-    N    CO
H        O-CH2-C≡C-CH3           -CH2-CH＝CH-CH2-    N    CO
H        OCH2-CH＝CH-Cl            -CH2-CH＝CH-CH2-    N    CO
H        O-CH(CH3)C≡CH            -CH2-CH＝CH-CH2-    N    CO
H        OCH(CH3)C≡C-H3          -CH2-CH＝CH-CH2-    N    CO
H        O-CH(CH3)CH＝CH2         -CH2-CH＝CH-CH2-    N    CO
H        OCH2CH＝CH-CH3           -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                   A                       E    G
H        O-CH3                -CH2-CH＝CH-CH2-      N    CO
H        O-C2H5              -CH2-CH＝CH-CH2-      N    CO
H        O-C3H7              -CH2-CH＝CH-CH2-      N    CO
H        O-C3H7-iso          -CH2-CH＝CH-CH2-      N    CO
H        
Figure C9411730300501
          -CH2-CH＝CH-CH2-      N    CO
H        
Figure C9411730300502
            -CH2-CH＝CH-CH2-      N    CO
H        O-CH(CH2F)2         -CH2-CH＝CH-CH2-      N    CO
H        OCH2-C(CH3)＝CH2   -CH2-CH＝CH-CH2-      N    CO
H                   -CH2-CH＝CH-CH2-      N    CO
H        
Figure C9411730300504
        -CH2-CH＝CH-CH2-      N    CO表1(续)
R1      R2                      A                     E    G
H        
Figure C9411730300511
            -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300512
            -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300513
            -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300514
         -CH2-CH＝CH-CH2-    N    CO
H        S-CH2-COOC5H11-n      -CH2-CH＝CH-CH2-    N    CO
H                   -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300516
          -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                            A                     E    G
H        O-CH2CH2-OCH(CH2F)2       -CH2-CH＝CH-CH2-    N    CO
H        S-CH(CH3)2                   -CH2-CH＝CH-CH2-    N    CO
H        O-CH2-CCl＝CH2               -CH2-CH＝CH-CH2-    N    CO
H                             -CH2-CH＝CH-CH2-    N    CO
H        O-CH2CN                       -CH2-CH＝CH-CH2-    N    CO
H        O-CH2COOC2H4-OCH3         -CH2-CH＝CH-CH2-    N    CO
H        O-CH2-COO-CH(CH3)COOC2H5  -CH2-CH＝CH-CH2-    N    CO
H        OCH2-COOCH2-COOC2H5       -CH2-CH＝CH-CH2-    N    CO
H        O-CHF2                        -CH2-CH＝CH-CH2-    N    CO
H        O-CH2CH2-OCH2CF3          -CH2-CH＝CH-CH2-    N    CO
H        NHCH3                         -CH2-CH＝CH-CH2-    N    CO
H        NHC2H5                       -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                     A                     E    G
H        N(CH3)2               -CH2-CH＝CH-CH2-    N    CO
H        NH-CH2-COOC2H5       -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300531
              CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300532
               -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2CH3             -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2C2H5           -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2C3H7-n         -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2C3H7-i         -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2C4H9-n         -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2C8H17-n        -CH2-CH＝CH-CH2-    N    CO
H        NH-COCH3               -CH2-CH＝CH-CH2-    N    CO表1(续)
R1      R2                        A                     E    G
H        NH-COC2H5                -CH2-CH＝CH-CH2-    N    CO
H        NH-COCF3                  -CH2-CH＝CH-CH2-    N    CO
H        N(CH3)-SO2CH3           -CH2-CH＝CH-CH2-    N    CO
H        N(CH3)-SO2C2H5         -CH2-CH＝CH-CH2-    N    CO
H        N(CH3)-SO2C3H7-n       -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2CF3                -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300541
               -CH2-CH＝CH-CH2-    N    CO
H        NH-SO2-C4F9-n           -CH2-CH＝CH-CH2-    N    CO
H        N(CH3)SO2CF3            -CH2-CH＝CH-CH2-    N    CO
H        
Figure C9411730300542
           -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                        A                     E    G
H                -CH2-CH＝CH-CH2-    N    CO
H            -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2CF3                -CH2-CH＝CH-CH2-    N    CO
Cl        OCF3                    -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2CH(CH3)-OC2H5   -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300553
             -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2-CH＝CH2           -CH2-CH＝CH-CH2-    N    CO
Cl        OH                       -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2-C≡CH              -CH2-CH＝CH-CH2-    N    CO
Cl        SCH2C＝CH               -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                        A                      E    G
Cl        OCH2COOC2H5             -CH2-CH＝CH-CH2-    N    CO
Cl        S-C(CH3)3                -CH2-CH＝CH-CH2-    N    CO
Cl        O-2-COOC5H11-n           -CH2-CH＝CH-CH2-    N    CO
Cl        OCH(CH3)-COOC2H5        -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2CH2-OCH3            -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2CH2-OC2H5          -CH2-CH＝CH-CH2-    N    CO
Cl        O(CH2CH2O)2-OC2H5    -CH2-CH＝CH-CH2-    N    CO
Cl        S-C3H7-n                 -CH2-CH＝CH-CH2-    N    CO
Cl        S-C2H5                   -CH2-CH＝CH-CH2-    N    CO
Cl        S-CH3                     -CH2-CH＝CH-CH2-    N    CO
Cl        S-CH2COOC2H5           -CH2-CH＝CH-CH2-    N    CO
Cl        SCH2CH2-COOC2H5       -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2-C≡C-CH3           -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                       A                     E    G
Cl        OCH2-CH＝CH-Cl           -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH(CH3)C≡CH           -CH2-CH＝CH-CH2-    N    CO
Cl        OCH(CH3)C≡C-CH3        -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH(CH3)CH＝CH2        -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2CH＝CH-H3           -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH3                    -CH2-CH＝CH-CH2-    N    CO
Cl        O-C2H5                  -CH2-CH＝CH-CH2-    N    CO
Cl        O-C3H7-n                -CH2-CH＝CH-CH2-    N    CO
Cl        O-C3H7-iso              -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300571
               -CH2-CH＝CH-CH2-    N    CO表1(续)
R1         R2                       A                     E    G
Cl          
Figure C9411730300581
               -CH2-CH＝CH-CH2-    N    CO
Cl          O-CH(CH2F)2            -CH2-CH＝CH-CH2-    N    CO
Cl          O-CH2-C(CH3)＝CH2     -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300582
             -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300583
           -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300584
        -CH2-CH＝CH-CH2-    N    CO
Cl                        -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300586
             -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                       A                     E    G
Cl        
Figure C9411730300591
       -CH2-CH＝CH-CH2-    N    CO
Cl        S-CH2-COOC5H11-n      -CH2-CH＝CH-CH2-    N    CO
Cl                  -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300593
           -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2CH2-OCH(CH2F)2 -CH2-CH＝CH-CH2-    N    CO
Cl        S-CH(CH3)2            -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2-CCl＝CH2        -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300594
          -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2CN                -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2COOC2H4-OCH3  -CH2-CH＝CH-CH2-    N    CO表1(续)
R1       R2                            A                     E    G
Cl        O-CH2-COO-CH(CH3)COOC2H5  -CH2-CH＝CH-CH2-    N    CO
Cl        OCH2-COOCH2-COOC2H5       -CF2-CH＝CH-CH2-    N    CO
Cl        O-CHF2                        -CH2-CH＝CH-CH2-    N    CO
Cl        O-CH2CH2-OCH2CF3          -CH2-CH＝CH-CH2-    N    CO
Cl        NHCH3                         -CH2-CH＝CH-CH2-    N    CO
Cl        NHC2H5                       -CH2-CH＝CH-CH2-    N    CO
Cl        N(CH3)2                      -CH2-CH＝CH-CH2-    N    CO
Cl        NFH-CH2-COOC2H5             -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300601
                        -CH2-CH＝CH-CH2-    N    CO
Cl        
Figure C9411730300602
                       -CH2-CH＝CH-CH2-    N    CO表1(续)
R1            R2                     A                     E    G
Cl             NH-SO2CH3             -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2C2H5           -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2C3H7-n         -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2C3H7-i         -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2C4H9-n         -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2C8H17-n         -CH2-CH＝CH-CH2-    N    CO
Cl             NH-COCH3                -CH2-CH＝CH-CH2-    N    CO
Cl             NH-COC2H5              -CH2-CH＝CH-CH2-    N    CO
Cl             NH-COCF3                -CH2-CH＝CH-CH2-    N    CO
Cl             N(CH3)-SO2CH3        -CH2-CH＝CH-CH2-    N    CO
Cl             N(CH3)-SO2C2H5      -CH2-CH＝CH-CH2-    N    CO
Cl             N(CH3)-SO2C3H7-n    -CH2-CH＝CH-CH2-    N    CO
Cl             NH-SO2CF3              -CH2-CH＝CH-CH2-    N    CO表1(续)
R1         R2                       A                     E    G
Cl          
Figure C9411730300621
             -CH2-CH＝CH-CH2-    N    CO
Cl          NH-SO2-C4F9-n         -CH2-CH＝CH-CH2-    N    CO
Cl          N(CH3)SO2CF3          -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300622
    -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300623
        -CH2-CH＝CH-CH2-    N    CO
Cl          
Figure C9411730300624
 -CH2-CH＝CH-CH2-    N    CO
F           O-CH(CH2F)2            -(CH2)2-CH＝CH-     N    CO
F           O-CH2-C(CH3)＝CH2     -(CH2)2-CH＝CH-     N    CO
F           
Figure C9411730300625
             -(CH2)2-CH＝CH-     N    CO表1(续)
R1          R2                      A                   E    G
F            
Figure C9411730300631
         -(CH2)2-CH＝CH-   N    CO
F            
Figure C9411730300632
         -(CH2)2-CH＝CH-    N    CO
F            
Figure C9411730300633
         -(CH2)2-CH＝CH-    N    CO
F                          -(CH2)2-CH＝CH-    N    CO
F            
Figure C9411730300635
      -(CH2)2-CH＝CH-    N    CO
F            S-CH2-COOC5H11-n     -(CH2)2-CH＝CH-    N    CO
F            
Figure C9411730300636
          -(CH2)2-CH＝CH-    N    CO表1(续)
R1      R2                            A                     E    G
F        
Figure C9411730300641
                  -(CH2)2-CH＝CH-    N    CO
F        O-CH2CH2-OCH(CH2F)2        -(CH2)2-CH＝CH-    N    CO
F        S-CH(CH3)2                   -(CH2)2-CH＝CH-    N    CO
F        O-CH2-CCl＝CH2               -(CH2)2-CH＝CH-    N    CO
F        
Figure C9411730300642
                     -(CH2)2-CH＝CH-    N    CO
F        O-CH2CN                        -(CH2)2-CH＝CH-    N    CO
F        O-CH2COOC2H4-OCH3          -(CH2)2-CH＝CH-    N    CO
F        O-CH2-COO-CH(CH3)COCC2H5   -(CH2)2-CH＝CH-    N    CO
F        OCH2-COOCH2-COOC2H5        -(CH2)2-CH＝CH-    N    CO
F        O-CHF2                         -(CH2)2-CH＝CH     N    CO表1(续)
R1        R2                        A                    E    G
F          O-CH2CH2-OCH2CF3       -(CH2)2-CH＝CH-   N    CO
F          OCH2CF3                  -(CH2)2-CH＝CH-    N    CO
F          OC3                       -(CH2)2-CH＝CH-    N    CO
F          OCH2CH(CH3)-OC2H5      -(CH2)2-CH＝CH-   N    CO
F          
Figure C9411730300651
              -(CH2)2-CH＝CH-    N    CO
F          OCH2-CH＝CH2             -(CH2)2-CH＝CH-    N    CO
F          OH                         -(CH2)2-CH＝CH-    N    CO
F          OCH2-C≡CH                -(CH2)2-CH＝CH-    N    CO
F          SCH2C≡CH                 -(CH2)2-CH＝CH-    N    CO
F          OCH2COOC2H5             -(CH2)2-CH＝CH-    N    CO
F          S-C(CH3)3                -(CH2)2-CH＝CH-    N    CO
F          OCH2-COOC5H11-n         -(CH2)2-CH＝CH-    N    CO
F          OCH(CH3)-COOC2H5        -(CH2)2-CH＝CH-    N    CO表1(续)
R1          R2                        A                    E    G
F            OCH2CH2-OCH3           -(CH2)2-CH＝CH-    N    CO
F            OCH2CH2-OC2H5         -(CH2)2-CH＝CH-    N    CO
F            O(CH2CH2O)2-OC2H5   -(CH2)2-CH＝CH-    N    CO
F            S-C3H7-n                -(CH2)2-CH＝CH-    N    CO
F            S-C2H5                  -(CH2)2-CH＝CH-    N    CO
F            S-CH3                    -(CH2)2-CH＝CH-    N    CO
F            S-CH2COOC2H5           -(CH2)2-CH＝CH-    N    CO
F            SCH2CH2-COOC2H5      -(CH2)2-CH＝CH-    N    CO
F            O-CH2-C＝C-CH3          -(CH2)2-CH＝CH-    N    CO
F            OCH2-CH＝CH-Cl           -(CH2)2-CH＝CH-    N    CO
F            O-CH(CH3)C＝CH           -(CH2)2-CH＝CH-    N    CO表1(续)
R1         R2                     A                      E    G
F           OCH(CH3)C≡C-CH3      -(CH2)2-CH＝CH-     N    CO
F           O-CH(CH3)CH＝CH2      -(CH2)2-CH＝CH-     N    CO
F           OCH2CH＝CH-CH3        -(CH2)2-CH＝CH-     N    CO
F           O-CH3                  -(CH2)2-CH＝CH-     N    CO
F           O-C2H5                -(CH2)2-CH＝CH-     N    CO
F           O-C3H7-n              -(CH2)2-CH＝CH-     N    CO
F           O-C3H7-iso            -(CH2)2-CH＝CH-     N    CO
F         
Figure C9411730300671
           -(CH2)2-CH＝CH-     N    CO
F         
Figure C9411730300672
            -(CH2)2-CH＝CH-     N    CO
F           NHCH3                  -(CH2)2-CH＝CH-     N    CO
F           NHC2H5                -(CH2)2-CH＝CH-     N    CO表1(续)
R1            R2                      A                    E    G
F             N(CH3)2                -(CH2)2-CH＝CH-    N    CO
F             NH-CH2-COOC2H5        -(CH2)2-CH＝CH-    N    CO
F             
Figure C9411730300681
                  -(CH2)2-CH＝CH-    N    CO
F             
Figure C9411730300682
                  -(CH2)2-CH＝CH-    N    CO
F             NH-SO2CH3              -(CH2)2-CH＝CH-    N    CO
F             NH-SO2C2H5            -(CH2)2-CH＝CH-    N    CO
F             NH-SO2C3H7-n          -(CH2)2-CH＝CH-    N    CO
F             NH-SO2C3H7-i          -(CH2)2-CH＝CH-    N    CO
F             NH-SO2C4H9-n          -(CH2)2-CH＝CH-    N    CO
F             NH-SO2C8H17-n         -(CH2)2-CH＝CH-    N    CO
F             NH-COCH3                -(CH2)2-CH＝CH-    N    CO
F             NH-COC2H5              -(CH2)2-CH＝CH-    N    CO表1(续)
R1          R2                        A                    E    G
F            NH-COCF3                  -(CH2)2-CH＝CH-    N    CO
F            N(CH3)-SO2CH3          -(CH2)2-CH＝CH-    N    CO
F            N(CH3)-SO2C2H5        -(CH2)2-CH＝CH-    N    CO
F            N(CH3)-SO2C3H7-n      -(CH2)2-CH＝CH-    N    CO
F            NH-SO2CF3               -(CH2)2-CH＝CH-    N    CO
F                           -(CH2)2-CH＝CH-    N    CO
F            NH-SO2-C4F9-n          -(CH2)2-CH＝CH-    N    CO
F            N(CH3)SO2CF3           -(CH2)2-CH＝CH-    N    CO
F            
Figure C9411730300692
           -(CH2)2-CH＝CH-    N    CO
F            
Figure C9411730300693
        -(CH2)2-CH＝CH-    N    CO表1(续)
R1           R2                        A                    E    G
F                  -(CH2)2-CH＝CH-    N    CO
H            OCH2CF3                   -(CH2)2-CH＝CH-    N    CO
H            OCF3                       -(CH2)2-CH＝CH-    N    CO
H            OCH2CH(CH3)-OC2H5      -(CH2)2-CH＝CH-    N    CO
H            
Figure C9411730300702
               -(CH2)2-CH＝CH-     N    CO
H            OCH2-CH＝CH2              -(CH2)2-CH＝CH-    N    CO
H            OH                          -(CH2)2-CH＝CH-    N    CO
H            OCH2-C≡CH                 -(CH2)2-CH＝CH-    N    CO
H            SCH2C≡CH                  -(CH2)2-CH＝CH-    N    CO
H            OCH2COOC2H5             -(CH2)2-CH＝CH-    N    CO表1(续)
R1          R2                     A                    E    G
H            S-C(CH3)3             -(CH2)2-CH＝CH-    N    CO
H            OCH2-COOC5H11-n      -(CH2)2-CH＝CH-    N    CO
H            OCH(CH3)-COOC2H5     -(CH2)2-CH＝CH-    N    CO
H            OCH2CH2-OCH3         -(CH2)2-CH＝CH-    N    CO
H            OCH2CH2-OC2H5       -(CH2)2-CH＝CH-    N    CO
H            O(CH2CH2O)2-OC2H5  -(CH2)2-CH＝CH-    N    CO
H            S-C3H7-n               -(CH2)2-CH＝CH-    N    CO
H            S-C2H5                 -(CH2)2-CH＝CH-    N    CO
H            S-CH3                   -(CH2)2-CH＝CH-    N    CO
H            S-CH2COOC2H5         -(CH2)2-CH＝CH-    N    CO
H            SCH2CH2-COOC2H5     -(CH2)2-CH＝CH-    N    CO
H            O-CH2-C＝C-CH3         -(CH2)2-CH＝CH-    N    CO
H            OCH2-CH＝CH-Cl          -(CH2)2-CH＝CH-    N    CO
H            O-CH(CH3)C≡CH          -(CH2)2-CH＝CH-    N    CO表1(续)
R1          R2                     A                    E    G
H            OCH(CH3)C≡C-CH3     -(CH2)2-CH＝CH-    N    CO
H            O-CH(CH3)CH＝CH2     -(CH2)2-CH＝CH-    N    CO
H            OCH2CH＝CH-CH3       -(CH2)2-CH＝CH-    N    CO
H            O-CH3                 -(CH2)2-CH＝CH-    N    CO
H            O-C2H5               -(CH2)2-CH＝CH-    N    CO
H            O-C3H7-n             -(CH2)2-CH＝CH-    N    CO
H            O-C3H7-iso           -(CH2)2-CH＝CH-    N    CO
H            
Figure C9411730300721
       -(CH2)2-CH＝CH-    N    CO表1(续)
R1           R2                    A                    E    G
H                       -(CH2)2-CH＝CH-    N    CO
H             O-CH(CH2F)2         -(CH2)2-CH＝CH-    N    CO
H             O-CH2-C(CH3)＝CH2  -(CH2)2-CH＝CH-    N    CO
H             
Figure C9411730300732
          -(CH2)2-CH＝CH-    N    CO
H                       -(CH2)2-CH＝CH-   N    CO
H                         -(CH2)2-CH＝CH-    N    CO
H                       -(CH2)2-CH＝CH-    N    CO
H                       -(CH2)2-CH＝CH-    N    CO
H             
Figure C9411730300737
       -(CH2)2-CH＝CH-    N    CO表1(续)
R1          R2                            A                    E    G
H            S-CH2-COOC5H11-n            -(CH2)2-CH＝CH-    N    CO
H            
Figure C9411730300741
                 -(CH2)2-CH＝CH-    N    CO
H                           -(CH2)2-CH＝CH-    N    CO
H            O-CH2CH2-OCH(CH2F)2        -(CH2)2-CH＝CH-    N    CO
H            S-CH(CH3)2                   -(CH2)2-CH＝CH-    N    CO
H            O-CH2-CCl＝CH2               -(CH2)2-CH＝CH-    N    CO
H            
Figure C9411730300743
                   -(CH2)2-CH＝CH-    N    CO
H            O-CH2CN                        -(CH2)2-CH＝CH-    N    CO
H            O-CH2COOC2H4-OCH3          -(CH2)2-CH＝CH-    N    CO
H            O-CH2-COO-CH(CH3)COOC2H5   -(CH2)2-CH＝CH-    N    CO
H            OCH2-COOCH2-COOC2H5        -(CH2)2-CH＝CH-    N    CO表1(续)
R1           R2                        A                    E    G
H             O-CHF2                    -(CH2)2-CH＝CH-    N    CO
H             O-CH2CH2-OCH2CF3      -(CH2)2-CH＝CH-    N    CO
H             NHCH3                     -(CH2)2-CH＝CH-    N    CO
H             NHC2H5                   -(CH2)2-CH＝CH-    N    CO
H             N(CH3)2                  -(CH2)2-CH＝CH-    N    CO
H             NH-CH2-COOC2H5          -(CH2)2-CH＝CH-    N    CO
H             
Figure C9411730300751
                    -(CH2)2-CH＝CH-    N    CO
H                                -(CH2)2-CH＝CH-    N    CO
H             NH-SO2CH3                -(CH2)2-CH＝CH-    N    CO
H             NH-SO2C2H5              -(CH2)2-CH＝CH-    N    CO
H             NH-SO2C3H7-n            -(CH2)2-CH＝CH-    N    CO
H             NH-SO2C3H7-i            -(CH2)2-CH＝CH-    N    CO表1(续)
R1            R2                      A                    E    G
H             NH-SO2C4H9-n          -(CH2)2-CH＝CH-    N    CO
H             NH-SO2C8H17-n         -(CH2)2-CH＝CH-    N    CO
H             NH-COCH3                -(CH2)2-CH＝CH-    N    CO
H             NH-COC2H5              -(CH2)2-CH＝CH-    N    CO
H             NH-COCF3                -(CH2)2-CH＝CH-    N    CO
H             N(CH3)-SO2CH3        -(CH2)2-CH＝CH-    N    CO
H             N(CH3)-SO2C2H5      -(CH2)2-CH＝CH-    N    CO
H             N(CH3)-SO2C3H7-n    -(CH2)2-CH＝CH-    N    CO
H             NH-SO2CF3              -(CH2)2-CH＝CH-    N    CO
H             
Figure C9411730300761
           -(CH2)2-CH＝CH-    N    CO表1(续)
R1       R2                       A                    E    G
H         NH-SO2-C4F9-n         -(CH2)2-CH＝CH-    N    CO
H         N(CH3)SO2CF3          -(CH2)2-CH＝CH-    N    CO
H                   -(CH2)2-CH＝CH-    N    CO
H         
Figure C9411730300772
        -(CH2)2-CH＝CH-    N    CO
H             -(CH2)2-CH＝CH-    N    CO
Cl        OCH2CF3                -(CH2)2-CH＝CH-    N    CO
Cl        OCF3                    -(CH2)2-CH＝CH-    N    CO
Cl        OCH2CH(CH3)-OC2H5   -(CH2)2-CH＝CH-    N    CO
Cl                 -(CH2)2-CH＝CH-    N    CO
Cl        OCH2-CH＝CH2          -(CH2)2-CH＝CH-    N    CO表1(续)
R1           R2                    A                    E    G
Cl            OH                     -(CH2)2-CH＝CH-    N    CO
Cl            OCH2-C≡CH            -(CH2)2-CH＝CH-    N    CO
Cl            SCH2C≡CH             -(CH2)2-CH＝CH-    N    CO
Cl            OCH2COOC2H5         -(CH2)2-CH＝CH-    N    CO
Cl            S-C(CH3)3            -(CH2)2-CH＝CH-    N    CO
Cl            OCH2-COOC5H11-n     -(CH2)2-CH＝CH-    N    CO
Cl            OCH(CH3)-COOC2H5    -(CH2)2-CH＝CH-    N    CO
Cl            OCH2CH2-OCH3        -(CH2)2-CH＝CH-    N    CO
Cl            OCH2CH2-OC2H5      -(CH2)2-CH＝CH-    N    CO
Cl            O(CH2CH2O)2-OC2H5 -(CH2)2-CH＝CH-    N    CO
Cl            S-C3H7-n              -(CH2)2-CH＝CH-    N    CO表1(续)
R1           R2                       A                     E    G
Cl            S-C2H5                  -(CH2)2-CH＝CH-    N    CO
Cl            S-CH3                    -(CH2)2-CH＝CH-    N    CO
Cl            S-CH2COOC2H5          -(CH2)2-CH＝CH-    N    CO
Cl            SCH2CH2-COOC2H5      -(CH2)2-CH＝CH-    N    CO
Cl            O-CH2-C≡CH3            -(CH2)2-CH＝CH-    N    CO
Cl            OCH2-CH＝CH-Cl           -(CH2)2-CH＝CH-    N    CO
Cl            O-CH(CH3)C≡CH           -(CH2)2-CH＝CH-    N    CO
Cl            OCH(CH3)C≡C-CH3        -(CH2)2-CH＝CH-    N    CO
Cl            O-CH(CH3)CH＝CH2        -(CH2)2-CH＝CH-    N    CO
Cl            OCH2CH＝CH-CH3          -(CH2)2-CH＝CH-    N    CO
Cl            O-CH3                    -(CH2)2-CH＝CH-    N    CO
Cl            O-C2H5                  -(CH2)2-CH＝CH-    N    CO
Cl            O-C3H7-n                -(CH2)2-CH＝CH-    N    CO
Cl            O-C3H7-iso              -(CH2)2-CH＝CH-    N    CO
Cl            
Figure C9411730300791
             -(CH2)2-CH＝CH-    N    CO表1(续)
R1       R2                      A                   E     G
Cl        
Figure C9411730300801
              -(CH2)2-CH＝CH-   N     CO
Cl        O-CH(CH2F)2           -(CH2)-CH＝CH-     N     CO
Cl        OCH2-C(CH3)＝CH2     -(CH2)-CH＝CH-     N     CO
Cl        
Figure C9411730300802
        -(CH2)-CH＝CH-     N     CO
Cl        
Figure C9411730300803
          -(CH2)-CH＝CH-     N     CO
Cl        
Figure C9411730300804
           -(CH2)-CH＝CH-     N     CO
Cl        
Figure C9411730300805
            -(CH2)-CH＝CH-     N     CO表1(续)
R1       R2                        A                 E    G
Cl        
Figure C9411730300811
         -(CH2)-CH＝CH-    N    CO
Cl        
Figure C9411730300812
        -(CH2)-CH＝CH-    N    CO
Cl        S-CH2-COOC5H11-n       -(CH2)-CH＝CH-    N    CO
Cl        
Figure C9411730300813
            -(CH2)-CH＝CH-    N    CO
Cl        
Figure C9411730300814
            -(CH2)-CH＝CH-    N    CO
Cl        O-CH2CH2-OCH(CH2F)2  -(CH2)-CH＝CH-    N    CO
Cl        S-CH(CH3)2              -(CH2)-CH＝CH-    N    CO
Cl        O-CH2-CCl＝CH2          -(CH2)-CH＝CH-    N    CO
Cl        
Figure C9411730300815
               -(CH2)-CH＝CH-    N    CO表1(续)
R1           R2                             A                  E    G
Cl            O-CH2CN                        -(CH2)-CH＝CH-    N    CO
Cl            O-CH2COOC2H4-OCH3          -(CH2)-CH＝CH-    N    CO
Cl            O-CH2-COO-CH(CH3)COOC2H5   -(CH2)-CH＝CH-    N    CO
Cl            OCH2-COOCH2-COOC2H5        -(CH2)-CH＝CH-    N    CO
Cl            O-CHF2                         -(CH2)-CH＝CH-    N    CO
Cl            O-CH2CH2-OCH2CF3           -(CH2)-CH＝CH-    N    CO
Cl            NHCH3                         -(CH2)-CH＝CH-    N    CO
Cl            NHC2H5                       -(CH2)-CH＝CH-    N    CO
Cl            N(CH3)2                      -(CH2)-CH＝CH-    N    CO
Cl            NH-CH2-COOC2H5              -(CH2)-CH＝CH-    N    CO
Cl            
Figure C9411730300821
                        -(CH2)-CH＝CH-    N    CO表1(续)
R1        R2                    A                   E    G
Cl         
Figure C9411730300831
              -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2CH3            -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2C2H5          -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2C3H7-n        -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2C3H7-i        -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2C4H9-n        -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2C8H17-n       -(CH2)-CH＝CH-    N    CO
Cl         NH-COCH3              -(CH2)-CH＝CH-    N    CO
Cl         NH-COC2H5            -(CH2)-CH＝CH-    N    CO
Cl         NH-COCF3              -(CH2)-CH＝CH-    N    CO
Cl         N(CH3)-SO2CH3       -(CH2)-CH＝CH-    N    CO
Cl         N(CH3)-SO2C2H5    -(CH2)-CH＝CH-    N    CO表1(续)
R1        R2                          A                 E    G
Cl         N(CH3)-SO2C3H7-n        -(CH2)-CH＝CH-   N    CO
Cl         NH-SO2CF3                 -(CH2)-CH＝CH-    N    CO
Cl         
Figure C9411730300841
               -(CH2)-CH＝CH-    N    CO
Cl         NH-SO2-C4F9-n            -(CH2)-CH＝CH-    N    CO
Cl         N(CH3)SO2CF3             -(CH2)-CH＝CH-    N    CO
Cl                   -(CH2)-CH＝CH-    N    CO
Cl         
Figure C9411730300843
         -(CH2)-CH＝CH-    N    CO
Cl         
Figure C9411730300844
     -(CH2)-CH＝CH-    N    CO表1(续)
R1          R2                               A              E        G
F            O-CH(CH2F)2                     -(CH2)4-       ＝N-
F            O-CH2-C(CH3)＝H2               -(CH2)4-      ＝N-
F            
Figure C9411730300853
                     -(CH2)4-       ＝N-
F            
Figure C9411730300855
                   -(CH2)4-   
Figure C9411730300856
   ＝N-
F            
Figure C9411730300857
                      -(CH2)4-   
Figure C9411730300858
   ＝N-
F            
Figure C9411730300859
                    -(CH2)4-   
Figure C94117303008510
    ＝N-
F                                  -(CH2)4-   
Figure C94117303008512
   ＝N-表1(续)
R1         R2                     A              E               G
F                 -(CH2)4-     
Figure C9411730300862
         ＝N-
F           S-CH2-COOC5H11-n    -(CH2)4-     
Figure C9411730300863
         ＝N-
F               -(CH2)4-     
Figure C9411730300865
         ＝N-
F                     -(CH2)4-               ＝N-
F          O-CH2CH2-OCH(CH2F)2 -(CH2)4-               ＝N-
F          S-CH(CH3)2            -(CH2)4-               ＝N-
F          O-CH2-CCl＝CH2        -(CH2)4-               ＝N-表1(续)
R1            R2                            A              E           G
F              
Figure C9411730300871
                  -(CH2)4-    
Figure C9411730300872
     ＝N-
F              O-CH2CN                       -(CH2)4-    
Figure C9411730300873
     ＝N-
F              O-CH2COOC2H4-OCH3          -(CH2)4-          ＝N-
F              O-CH2-COO-CH(CH3)COOC2H5   -(CH2)4-    
Figure C9411730300875
     ＝N-
F              OCH2-COOCH2-COOC2H5        -(CH2)4-    
Figure C9411730300876
     ＝N-
F              O-CHF2                        -(CH2)4-    
Figure C9411730300877
     ＝N-
F              O-CH2CH2-OCH2CF3           -(CH2)4-    
Figure C9411730300878
     ＝N-
F              OCH2CF3                      -(CH2)4-    
Figure C9411730300879
     ＝N-表1(续)
R1        R2                     A               E            G
F          OCF3                   -(CH2)4-      
Figure C9411730300881
      ＝N-
F          OCH2CH(CH3)-OC2H5  -(CH2)4-      
Figure C9411730300882
     ＝N-
F          
Figure C9411730300883
         -(CH2)4-             ＝N-
F          OCH2-CH＝CH2          -(CH2)4-      
Figure C9411730300885
      ＝N-
F          OH                      -(CH2)4-             ＝N-
F          OCH2-C＝CH             -(CH2)4-             ＝N-
F          SCH2C＝CH              -(CH2)4-             ＝N-
F          OCH2COOC2H5          -(CH2)4-      
Figure C9411730300889
     ＝N-表1(续)
R1          R2                    A              E              G
F            S-C(CH3)3            -(CH2)4-     
Figure C9411730300891
      ＝N-
F            OCH2-COOC5H11-n     -(CH2)4-          ＝N-
F            OCH(CH3)-COOC2H5    -(CH2)4-     
Figure C9411730300893
      ＝N-
F            OCH2CH2-OCH3        -(CH2)4-     
Figure C9411730300894
      ＝N-
F            OCH2CH2-OC2H5      -(CH2)4-     
Figure C9411730300895
      ＝N-
F            O(CH2CH2O)2-OC2H5 -(CH2)4-     
Figure C9411730300896
      ＝N-
F            S-C3H7-n             -(CH2)4-     
Figure C9411730300897
       ＝N-
F            S-C2H5               -(CH2)4-     
Figure C9411730300898
       ＝N-表1(续)
R1            R2                     A             E          G
F              S-CH3                 -(CH2)4-          ＝N-
F              S-CH2COOC2H5        -(CH2)4-    
Figure C9411730300902
    ＝N-
F              SCH2CH2-COOC2H5    -(CH2)4-    
Figure C9411730300903
     ＝N-
F              O-CH2-C＝C-CH3       -(CH2)4-          ＝N-
F              OCH2-CH＝CH-Cl        -(CH2)4-    
Figure C9411730300905
     ＝N-
F              O-CH(CH3)C≡CH        -(CH2)4-          ＝N-
F              OCH(CH3)C≡C-CH3     -(CH2)4-    
Figure C9411730300907
     ＝N-
F              O-CH(CH3)CH＝CH2     -(CH2)4-    
Figure C9411730300908
    ＝N-表1(续)
R1       R2                     A              E          G
F         OCH2CH＝CH-CH3        -(CH2)4-     
Figure C9411730300911
    ＝N-
F         O-CH3                  -(CH2)4-          ＝N-
F         O-C2H5                -(CH2)4-          ＝N-
F         O-C3H7-n              -(CH2)4-          ＝N-
F         O-C3H7-iso            -(CH2)4-     
Figure C9411730300915
    ＝N-
F         
Figure C9411730300916
        -(CH2)4-     
Figure C9411730300917
    ＝N-
F                       -(CH2)4-     
Figure C9411730300919
    ＝N-
F        NHCH3                   -(CH2)4-    
Figure C94117303009110
    ＝N-表1(续)
R1         R2                 A                E          G
F          NHC2H5            -(CH2)4-       
Figure C9411730300921
    ＝N-
F          N(CH3)2           -(CH2)4-           ＝N-
F          NH-CH2-COOC2H5   -(CH2)4-            ＝N-
F          
Figure C9411730300924
            -(CH2)4-       
Figure C9411730300925
    ＝N-
F                      -(CH2)4-       
Figure C9411730300927
    ＝N-
F         NH-SO2CH3          -(CH2)4-       
Figure C9411730300928
    ＝N-
F         NH-SO2C2H5        -(CH2)4-       
Figure C9411730300929
    ＝N-
F         NH-SO2C3H7-n      -(CH2)4-       
Figure C94117303009210
   ＝N-表1(续)
R1           R2                      A              E           G
F             NH-SO2C3H7-i          -(CH2)4-          ＝N-
F             NH-SO2C4H9-n          -(CH2)4-    
Figure C9411730300932
    ＝N-
F             NH-SO2C8H17-n         -(CH2)4-     
Figure C9411730300933
    ＝N-
F             NH-COCH3                -(CH2)4-     
Figure C9411730300934
    ＝N-
F             NH-COC2H5              -(CH2)4-          ＝N-
F             NH-COCF3                -(CH2)4-          ＝N-
F             N(CH3)-SO2CH3         -(CH2)4-     
Figure C9411730300937
    ＝N-
F             N(CH3)-SO2C2H5       -(CH2)4-    
Figure C9411730300938
    ＝N-表1(续)
R1        R2                        A              E           G
F          N(CH3)-SO2C3H7-n       -(CH2)4-    
Figure C9411730300941
     ＝N-
F          NH-SO2CF3                -(CH2)4-         ＝N-
F          
Figure C9411730300943
              -(CH2)4-     
Figure C9411730300944
     ＝N-
F          NH-SO2-C4F9-n           -(CH2)4-           ＝N-
F          N(CH3)SO2CF3            -(CH2)4-     
Figure C9411730300946
     ＝N-
F          
Figure C9411730300947
            -(CH2)4-           ＝N-
F                    -(CH2)4-           ＝N-表1(续)
R1              R2                      A              E            G
F                  -(CH2)4-     
Figure C9411730300952
    ＝N-
H                OCH2CF3                -(CH2)4-     
Figure C9411730300953
    ＝N-
H                OCF3                    -(CH2)4-     
Figure C9411730300954
    ＝N-
H                OCH2CH(CH3)-OC2H5   -(CH2)4-          ＝N-
H                            -(CH2)4-     
Figure C9411730300957
    ＝N-
H                OCH2-CH＝CH2           -(CH2)4-     
Figure C9411730300958
    ＝N-
H                OH                       -(CH2)4-          ＝N-
H                OCH2-C≡CH              -(CH2)4-     
Figure C94117303009510
   ＝N-表1(续)
R1           R2                   A              E              G
H            SCH2C≡CH             -(CH2)4-     
Figure C9411730300961
      ＝N-
H            OCH2COOC2H5         -(CH2)4-     
Figure C9411730300962
    ＝N-
H            S-C(CH3)3            -(CH2)4-            ＝N-
H            OCH2-COOC5H11-n     -(CH2)4-            ＝N-
H            OCH(CH3)-COOC2H5    -(CH2)4-            ＝N-
H            OCH2CH2-OCH3        -(CH2)4-     
Figure C9411730300966
      ＝N-
H            OCH2CH2-OC2H5      -(CH2)4-            ＝N-
H            O(CH2CH2O)2-OC2H5 -(CH2)4-     
Figure C9411730300968
     ＝N-表1(续)
R1          R2                     A              E            G
H            S-C3H7-n              -(CH2)4-     
Figure C9411730300971
     ＝N-
H            S-C2H5                -(CH2)4-           ＝N-
H            S-CH3                  -(CH2)4-     
Figure C9411730300973
     ＝N-
H            S-CH2COOC2H5         -(CH2)4-     
Figure C9411730300974
     ＝N-
H            SCH2CH2-COOC2H5     -(CH2)4-     
Figure C9411730300975
     ＝N-
H            O-CH2-C≡C-CH3        -(CH2)4-    
Figure C9411730300976
     ＝N-
H            OCH2-CH＝CH-Cl         -(CH2)4-            ＝N-表1(续)
R1       R2                  A                    E       G
H        O-CH(CH3)C≡CH        -(CH2)4-     
Figure C9411730300981
     ＝N-
H        OCH(CH3)C≡C-CH3    -(CH2)4-           ＝N-
H        O-CH(CH3)CH＝CH2    -(CH2)4-     
Figure C9411730300983
     ＝N-
H        OCH2CH＝CH-CH3      -(CH2)4-     
Figure C9411730300984
     ＝N-
H        O-CH3                -(CH2)4-     
Figure C9411730300985
     ＝N-
H        O-C2H5              -(CH2)4-     
Figure C9411730300986
  ＝N-
H        O-C3H7-n            -(CH2)4-     
Figure C9411730300987
     ＝N-
H        O-C3H7-iso          -(CH2)4-     
Figure C9411730300988
     ＝N-
H                 -(CH2)4-            ＝N-表1(续)
R1       R2                                  A                    E          G
H            
Figure C9411730300991
                       -(CH2)4-        
Figure C9411730300992
     ＝N-
H            O-CH(CH2F)2                     -(CH2)4-        
Figure C9411730300993
     ＝N-
H            O-CH2-C(CH3)＝CH2              -(CH2)4-        
Figure C9411730300994
     ＝N-
H            
Figure C9411730300995
                   -(CH2)4-        
Figure C9411730300996
     ＝N-
H                             -(CH2)4-              ＝N-
H            
Figure C9411730300999
                    -(CH2)4-        
Figure C94117303009910
     ＝N-
H            
Figure C94117303009911
                    -(CH2)4-       
Figure C94117303009912
    ＝N-表1(续)
R1      R2                         A                   E            G
H        
Figure C9411730301001
                -(CH2)4-        
Figure C9411730301002
     ＝N-
H        
Figure C9411730301003
           -(CH2)4-              ＝N-
H        S-CH2-COOC5H11-n        -(CH2)4-        
Figure C9411730301005
      ＝N-
H        
Figure C9411730301006
            -(CH2)4-               ＝N-
H                     -(CH2)4-        
Figure C9411730301009
      ＝N-
H        O-CH2CH2-OCH(CH2F)2    -(CH2)4-        
Figure C94117303010010
     ＝N-
H        S-CH(CH3)2               -(CH2)4-               ＝N-表1(续)
R1          R2                            A             E        G
H            O-CH2-CCl＝CH2              -(CH2)4-    
Figure C9411730301011
    ＝N-
H            
Figure C9411730301012
                   -(CH2)4-    
Figure C9411730301013
  ＝N-
H            O-CH2CN                       -(CH2)4-         ＝N-
H            O-CH2COOC2H4-OCH3         -(CH2)4-    
Figure C9411730301015
    ＝N-
H            O-CH2-COO-CH(CH3)COOC2H5  -(CH2)4-         ＝N-
H            OCH2-COOCH2-COOC2H5       -(CH2)4-    
Figure C9411730301017
    ＝N-
H            O-CHF2                       -(CH2)4-    
Figure C9411730301018
     ＝N-表1(续)
R1      R2                  A               E               G
H        O-CH2CH2-OCH2CF3 -(CH2)4-              ＝N-
H        NHCH3               -(CH2)4-      
Figure C9411730301022
       ＝N-
H        NHC2H5             -(CH2)4-      
Figure C9411730301023
       ＝N-
H        N(CH3)2            -(CH2)4-              ＝N-
H        NH-CH2-COOC2H5    -(CH2)4-      
Figure C9411730301025
       ＝N-
H        
Figure C9411730301026
          -(CH2)4-      
Figure C9411730301027
       ＝N-
H        
Figure C9411730301028
             -(CH2)4-      
Figure C9411730301029
       ＝N-
H         NH-SO2CH3         -(CH2)4-      
Figure C94117303010210
       ＝N-
H         NH-SO2C2H5       -(CH2)4-      
Figure C94117303010211
       ＝N-表1(续)
R1       R2                 A                E             G
H         NH-SO2C3H7-n     -(CH2)4-      
Figure C9411730301031
     ＝N-
H         NH-SO2C3H7-i     -(CH2)4-      
Figure C9411730301032
    ＝N-
H         NH-SO2C4H9-n     -(CH2)4-      
Figure C9411730301033
      ＝N-
H         NH-SO2C8H17-n    -(CH2)4-      
Figure C9411730301034
      ＝N-
H         NH-COCH3           -(CH2)4-      
Figure C9411730301035
      ＝N-
H         NH-COC2H5         -(CH2)4-             ＝N-表1(续)
R1      R2                      A              E              G
H        NH-COCF3                -(CH2)4-     
Figure C9411730301041
       ＝N-
H        N(CH3)-SO2CH3         -(CH2)4-     
Figure C9411730301042
     ＝N-
H        N(CH3)-SO2C2H5       -(CH2)4-     
Figure C9411730301043
      ＝N-
H        N(CH3)-SO2C3H7-n     -(CH2)4-     
Figure C9411730301044
       ＝N-
H        NH-SO2CF3              -(CH2)4-     
Figure C9411730301045
       ＝N-
H                     -(CH2)4-     
Figure C9411730301047
       ＝N-
H        NH-SO2-C4F9-n         -(CH2)4-            ＝N-
H        N(CH3)SO2CF3          -(CH2)4-     
Figure C9411730301049
     ＝N-
H        
Figure C94117303010410
         -(CH2)4-            ＝N-
H        
Figure C94117303010412
       -(CH2)4-            ＝CN-表1(续)
R1        R2                       A               E           G
H          
Figure C9411730301051
 -(CH2)4-       
Figure C9411730301052
     ＝N-
Cl         OCH2CF3                -(CH2)4-       
Figure C9411730301053
     ＝N-
Cl         OCF3                    -(CH2)4-       
Figure C9411730301054
     ＝N-
Cl         OCH2CH(CH3)-OC2H5    -(CH2)4-       
Figure C9411730301055
    ＝N-
Cl         
Figure C9411730301056
            -(CH2)4-       
Figure C9411730301057
     ＝N-
Cl         OCH2-CH＝CH2           -(CH2)4-             ＝N-
Cl         OH                       -(CH2)4-       
Figure C9411730301059
     ＝N-表1(续)
R1       R2                            A            E         G
Cl        OCH2-C≡CH                    -(CH2)4-      ＝N-
Cl        SCH2C≡CH                     -(CH2)4-     ＝N-
Cl        OCH2COOC2H5                 -(CH2)4-   
Figure C9411730301063
  ＝N-
Cl        S-C(CH3)3                    -(CH2)4-   
Figure C9411730301064
  ＝N-
Cl        OCH2-COOC5H11-n             -(CH2)4-   
Figure C9411730301065
  ＝N-
Cl        OCH(CH3)-COOC2H5            -(CH2)4-      ＝N-表1(续)
R1       R2                      A              E             G
C1        OCH2CH2-OCH3          -(CH2)4-            ＝N-
Cl        OCH2CH2-OC2H5        -(CH2)4-           ＝N-
C1        O(CH2CH2O)2-OC2H5   -(CH2)4-        ＝N-
Cl        S-C3H7-n               -(CH2)4-     
Figure C9411730301074
      ＝N-
Cl        S-C2H5                 -(CH2)4-     
Figure C9411730301075
      ＝N-
Cl        S-CH3                   -(CH2)4-            ＝N-表1(续)
R1       R2                       A              E            G
Cl        S-CH2COOC2H5           -(CH2)4-     
Figure C9411730301081
     ＝N-
Cl        SCH2CH2-COOC2H5       -(CH2)4-     
Figure C9411730301082
     ＝N-
Cl        O-CH2-C≡C-CH3          -(CH2)4-     
Figure C9411730301083
     ＝N-
Cl        OCH2-CH＝CH-Cl           -(CH2)4-     
Figure C9411730301084
     ＝N-
Cl        O-CH(CH3)C≡CH           -(CH2)4-     
Figure C9411730301085
     ＝N-
Cl        OCH(CH3)C≡C-CH3        -(CH2)4-     
Figure C9411730301086
     ＝N-表1(续)
R1       R2                        A             E            G
Cl        O-CH(CH3)CH＝CH2         -(CH2)4-    
Figure C9411730301091
     ＝N-
Cl        OCH2CH＝CH-CH3           -(CH2)4-    
Figure C9411730301092
   ＝N-
Cl        O-CH3                     -(CH2)4-    
Figure C9411730301093
     ＝N-
Cl        O-C2H5                   -(CH2)4-    
Figure C9411730301094
     ＝N-
Cl        O-C3H7-n                 -(CH2)4-    
Figure C9411730301095
     ＝N-
Cl        O-C3H7-iso               -(CH2)4-          ＝N-
Cl        
Figure C9411730301097
               -(CH2)4-          ＝N-
Cl        
Figure C9411730301099
                -(CH2)4-    
Figure C94117303010910
     ＝N-
Cl        O-CH(CH2F)2              -(CH2)4-    
Figure C94117303010911
     ＝N-
Cl        O-CH2-C(CH3)＝CH2       -(CH2)4-           ＝N-表1(续)
R1      R2                           A               E              G
Cl                      -(CH2)4-      
Figure C9411730301102
       ＝N-
Cl       
Figure C9411730301103
                -(CH2)4-              ＝N-
Cl       
Figure C9411730301105
             -(CH2)4-      
Figure C9411730301106
       ＝N-
Cl       
Figure C9411730301107
                -(CH2)4-               ＝N-
Cl       
Figure C9411730301109
                -(CH2)4-      
Figure C94117303011010
       ＝N-
Cl       
Figure C94117303011011
              -(CH2)4-      
Figure C94117303011012
       ＝N-
Cl       S-CH2-COOC5H11-n            -(CH2)4-    
Figure C94117303011013
       ＝N-表1(续)
R1      R2                        A               E            G
Cl                   -(CH2)4-             ＝N-
Cl                   -(CH2)4-            ＝N-
Cl       O-CH2CH2-OCH(CH2F)2  -(CH2)4-       
Figure C9411730301115
     ＝N-
Cl       S-CH(CH3)2             -(CH2)4-       
Figure C9411730301116
     ＝N-
Cl       O-CH2-CCl＝CH2         -(CH2)4-       
Figure C9411730301117
     ＝N-
Cl       
Figure C9411730301118
             -(CH2)4-       
Figure C9411730301119
     ＝N-
Cl       O-CH2CN                 -(CH2)4-             ＝N-
Cl       O-CH2COOC2H4-OCH3    -(CH2)4-       
Figure C94117303011111
    ＝N-表1(续)
R1       R2                           A                E        G
Cl        O-CH2-COO-CH(CH3)COOC2H5  -(CH2)4-         ＝N-
Cl        OCH2-COOCH2-COOC2H5       -(CH2)4-    
Figure C9411730301122
   ＝N-
Cl        O-CHF2                       -(CH2)4-          ＝N-
Cl        O-CH2CH2-OCH2CF3          -(CH2)4-         ＝N-
Cl        NHCH3                        -(CH2)4-          ＝N-
Cl        NHC2H5                      -(CH2)4-     
Figure C9411730301126
    ＝N-
Cl        N(CH3)2                     -(CH2)4-   
Figure C9411730301127
    ＝N-
Cl        NH-CH2-COOC2H5             -(CH2)4-   
Figure C9411730301128
     ＝N-表1(续)
R1      R2                      A              E           G
Cl                        -(CH2)4-           ＝N-
Cl       
Figure C9411730301133
               -(CH2)4-      
Figure C9411730301134
    ＝N-
Cl       NH-SO2CH3            -(CH2)4-      
Figure C9411730301135
    ＝N-
Cl       NH-SO2C2H5          -(CH2)4-           ＝N-
Cl       NH-SO2C3H7-n        -(CH2)4-           ＝N-
Cl       NH-SO2C3H7-i        -(CH2)4-           ＝N-
Cl       NH-SO2C4H9-n        -(CH2)4-      
Figure C9411730301139
    ＝N-
Cl       NH-SO2C8H17-n       -(CH2)4-      
Figure C94117303011310
    ＝N-表1(续)
R1         R2                     A              E               G
Cl          NH-COCH3               -(CH2)4-     
Figure C9411730301141
      ＝N-
Cl          NH-COC2H5             -(CH2)4-     
Figure C9411730301142
    ＝N-
Cl          NH-COCF3               -(CH2)4-     
Figure C9411730301143
      ＝N-
Cl          N(CH3)-SO2CH3        -(CH2)4-     
Figure C9411730301144
      ＝N-
Cl          N(CH3)-SO2C2H5      -(CH2)4-     
Figure C9411730301145
      ＝N-
Cl          -N(CH3)-SO2C3H7-n   -(CH2)4-     
Figure C9411730301146
      ＝N-
Cl          NH-SO2CF3             -(CH2)4-     
Figure C9411730301147
      ＝N-
Cl          
Figure C9411730301148
           -(CH2)4-     
Figure C9411730301149
      ＝N-表1(续)
R1       R2                      A               E        G
Cl        NH-SO2-C4F9-n        -(CH2)4-    
Figure C9411730301151
    ＝N-
Cl        N(CH3)SO2CF3         -(CH2)4-    
Figure C9411730301152
   ＝N-
Cl        
Figure C9411730301153
         -(CH2)4-         ＝N-
Cl               -(CH2)4-    
Figure C9411730301156
    ＝N-
Cl        
Figure C9411730301157
 -(CH2)4-    
Figure C9411730301158
    ＝N-
F        O-CH(CH2F)2            -(CH2)3-         ＝N-
F        O-CH2-C(CH3)＝CH2     -(CH2)3-         ＝N-
F                     -(CH2)3-    
Figure C94117303011512
    ＝N-表1(续)
R1      R2                               A             E          G
F        
Figure C9411730301161
          -(CH2)3-     
Figure C9411730301162
    ＝N-
F        
Figure C9411730301163
            -(CH2)3-     
Figure C9411730301164
   ＝N-
F        
Figure C9411730301165
                -(CH2)3-          ＝N-
F        
Figure C9411730301167
                   -(CH2)3-        ＝N-
F        
Figure C9411730301169
           -(CH2)3-      
Figure C94117303011610
    ＝N-
F        S-CH2-COOC5H11-n            -(CH2)3-      
Figure C94117303011611
   ＝N-
F        
Figure C94117303011612
                -(CH2)3-      
Figure C94117303011613
   ＝N-表1(续)R1          R2                            A                 E          G
F           
Figure C9411730301171
             -(CH2)3-           ＝N-
F        O-CH2CH2-OCH(CH2F)2       -(CH2)3-      
Figure C9411730301173
   ＝N-
F        S-CH(CH3)2                  -(CH2)3-       
Figure C9411730301174
   ＝N-
F        O-CH2-CCl＝CH2              -(CH2)3-           ＝N-
F                           -(CH2)3-       
Figure C9411730301177
   ＝N-
F        O-CH2CN                      -(CH2)3-           ＝N-
F        O-CH2COOC2H4-OCH3         -(CH2)3-           ＝N-
F        O-OH2-COO-CH(CH3)COOC2H5  -(CH2)3-       
Figure C94117303011710
   ＝N-表1(续)
R1      R2                            A               E          G
F        OCH2-COOCH2-COOC2H5       -(CH2)3-          ＝N-
F        O-CHF2                       -(CH2)3-     
Figure C9411730301182
    ＝N-
F        O-CH2CH2-OCH2CF3          -(CH2)3-          ＝N-
F        OCH2CF3                     -(CH2)3-     
Figure C9411730301184
    ＝N-
F        OCF3                         -(CH2)3-     
Figure C9411730301185
    ＝N-
F        OCH2CH(CH3)-OC2H5         -(CH2)3-     
Figure C9411730301186
    ＝N-
F                         -(CH2)3-     
Figure C9411730301188
    ＝N-
F        OCH2-CH＝CH2                -(CH2)3-          ＝N-表1(续)
R1          R2                        A                E            G
F            OH                         -(CH2)3-       
Figure C9411730301191
      ＝N-
F            OCH2-C≡CH                -(CH2)3-              ＝N-
F            SCH2C≡CH                 -(CH2)3-              ＝N-
F            OCH2COOC2H5             -(CH2)3-       
Figure C9411730301194
      ＝N-
F            S-C(CH3)3                -(CH2)3-       
Figure C9411730301195
      ＝N-
F            OCH2-COOC5H11-n         -(CH2)3-              ＝N-
F            OCH(CH3)-COOC2H5        -(CH2)3-       
Figure C9411730301197
      ＝N-
F            OCH2CH2-OCH3            -(CH2)3-              ＝N-表1(续)
R1      R2                      A              E         G
F        OCH2CH2-OC2H5        -(CH2)3-     
Figure C9411730301201
   ＝N-
F        O(CH2CH2O)2-OC2H5   -(CH2)3-     
Figure C9411730301202
   ＝N-
F        S-C3H7-n               -(CH2)3-     
Figure C9411730301203
   ＝N-
F        S-C2H5                 -(CH2)3-     
Figure C9411730301204
   ＝N-
F        S-CH3                   -(CH2)3-     
Figure C9411730301205
   ＝N-
F        S-CH2COOC2H5          -(CH2)3-         ＝N-
F        SCH2CH2-COOC2H5      -(CH2)3-     
Figure C9411730301207
   ＝N-
F        O-CH2-C≡C-CH3         -(CH2)3-     
Figure C9411730301208
   ＝N-表1(续)
R1      R2                         A              E          G
F        OCH2-CH＝CH-Cl             -(CH2)3-     
Figure C9411730301211
    ＝N-
F        O-CH(CH3)C≡CH             -(CH2)3-          ＝N-
F        OCH(CH3)C≡C-CH3          -(CH2)3-     
Figure C9411730301213
    ＝N-
F        O-CH(CH3)CH＝CH2          -(CH2)3-     
Figure C9411730301214
    ＝N-
F        OCH2CH＝CH-CH3            -(CH2)3-     
Figure C9411730301215
    ＝N-
F        O-CH3                      -(CH2)3-          ＝N-
F        O-C2H5                    -(CH2)3-     
Figure C9411730301217
    ＝N-
F        O-C3H7-n                  -(CH2)3-          ＝N-表1(续)
R1      R2                     A               E         G
F        O-C3H7-iso            -(CH2)3-         ＝N-
F        
Figure C9411730301222
           -(CH2)3-     
Figure C9411730301223
   ＝N-
F        
Figure C9411730301224
           -(CH2)3-         ＝N-
F        NHCH3                  -(CH2)3-         ＝N-
F        NHC2H5                -(CH2)3-         ＝N-
F        N(CH3)2               -(CH2)3-     
Figure C9411730301228
   ＝N-
F        NH-CH2-COOC2H5       -(CH2)3-     
Figure C9411730301229
   ＝N-
F                         -(CH2)3-         ＝N-表1(续)
R1       R2                      A              E               G
F                           -(CH2)3-    
Figure C9411730301232
         ＝N-
F         NH-SO2CH3              -(CH2)3-     
Figure C9411730301233
       ＝N-
F         NH-SO2C2H5            -(CH2)3-     
Figure C9411730301234
       ＝N-
F         NH-SO2C3H7-n          -(CH2)3-             ＝N-
F         NH-SO2C3H7-i          -(CH2)3-     
Figure C9411730301236
       ＝N-
F         NH-SO2C4H9-n          -(CH2)3-     
Figure C9411730301237
       ＝N-
F         NH-SO2C8H17-n         -(CH2)3-     
Figure C9411730301238
       ＝N-表1(续)
R1       R2                      A              E              G
F         NH-COCH3                -(CH2)3-             ＝N-
F         NH-COC2H5              -(CH2)3-             ＝N-
F         NH-COCF3                -(CH2)3-             ＝N-
F         N(CH3)-SO2CH3         -(CH2)3-     
Figure C9411730301244
       ＝N-
F         N(CH3)-SO2C2H5       -(CH2)3-     
Figure C9411730301245
       ＝N-
F         N(CH3)-SO2C3H7-n     -(CH2)3-     
Figure C9411730301246
       ＝N-
F         NH-SO2CF3              -(CH2)3-             ＝N-
F         
Figure C9411730301248
        -(CH2)3-             ＝N-
F         NH-SO2-C4F9-n        -(CH2)3-    
Figure C94117303012410
       ＝N-表1(续)
R1       R2                        A               E       G
F         N(CH3)SO2CF3            -(CH2)3-          ＝N-
F         
Figure C9411730301252
           -(CH2)3-   
Figure C9411730301253
     ＝N-
F         
Figure C9411730301254
        -(CH2)3-     
Figure C9411730301255
     ＝N-
F         
Figure C9411730301256
   -(CH2)3-     
Figure C9411730301257
     ＝N-
H         OCH2CF3                  -(CH2)3-           ＝N-
H         OCF3                      -(CH2)3-     
Figure C9411730301259
     ＝N-
H         OCH2CH(CH3)-OC2H5      -(CH2)3-           ＝N-表4(续)
R1      R2                       A              E           G
H                     -(CH2)3-           ＝N-
H        OCH2-CH＝CH2            -(CH2)3-           ＝N-
H        OH                        -(CH2)3-     
Figure C9411730301264
     ＝N-
H        OCH2-C＝CH               -(CH2)3-     
Figure C9411730301265
     ＝N-
H        SCH2C≡CH                -(CH2)3-     
Figure C9411730301266
     ＝N-
H        OCH2COOC2H5            -(CH2)3-     
Figure C9411730301267
     ＝N-
H        S-C(CH3)3               -(CH2)3-     
Figure C9411730301268
     ＝N-
H        OCH2-COOC5H11-n        -(CH2)3-     
Figure C9411730301269
    ＝N-表1(续)
R1      R2                          A              E            G
H        OCH(CH3)-COOC2H5        -(CH2)3-           ＝N-
H        OCH2CH2-OCH3            -(CH2)3-           ＝N-
H        OCH2CH2-OC2H5          -(CH2)3-     
Figure C9411730301273
     ＝N-
H        O(CH2CH2O)2-OC2H5     -(CH2)3-     
Figure C9411730301274
    ＝N-
H        S-C3H7-n                 -(CH2)3-     
Figure C9411730301275
      ＝N-
H        S-C2H5                   -(CH2)3-     
Figure C9411730301276
  ＝N-
H        S-CH3                     -(CH2)3-           ＝N-
H        S-CH2COOC2H5            -(CH2)3-     
Figure C9411730301278
     ＝N-
H        SCH2CH2-COOC2H5        -(CH2)3-     
Figure C9411730301279
     ＝N-表1(续)
R1        R2                      A              E           G
H          O-CH2-C≡C-CH3         -(CH2)3-     
Figure C9411730301281
     ＝N-
H          OCH2-CH＝CH-Cl          -(CH2)3-           ＝N-
H          O-CH(CH3)C≡CH          -(CH2)3-     
Figure C9411730301283
     ＝N-
H          OCH(CH3)C≡C-CH3       -(CH2)3-           ＝N-
H          O-CH(CH3)CH＝CH2       -(CH2)3-     
Figure C9411730301285
     ＝N-
H          OCH2CH＝CH-CH3         -(CH2)3-  
Figure C9411730301286
     ＝N-
H          O-CH3                   -(CH2)3-           ＝N-表1(续)
R1      R2                    A              E         G
H        O-C2H5               -(CH2)3-     
Figure C9411730301291
     ＝N-
H        O-C3H7-n             -(CH2)3-     
Figure C9411730301292
     ＝N-
H        O-C3H7-iso           -(CH2)3-           ＝N-
H        
Figure C9411730301294
        -(CH2)3-     
Figure C9411730301295
     ＝N-
H        
Figure C9411730301296
       -(CH2)3-     
Figure C9411730301297
     ＝N-
H        O-CH(CH2F)2          -(CH2)3-     
Figure C9411730301298
     ＝N-
H        O-CH2-C(CH3)＝CH2   -(CH2)3-     
Figure C9411730301299
     ＝N-表1(续)
R1       R2                              A                     E          G
H         
Figure C9411730301301
                  -(CH2)3-        
Figure C9411730301302
     ＝N-
H                            -(CH2)3-        
Figure C9411730301304
      ＝N-
H                            -(CH2)3-        
Figure C9411730301306
      ＝N-
H         
Figure C9411730301307
                  -(CH2)3-        
Figure C9411730301308
      ＝N-
H         
Figure C9411730301309
                  -(CH2)3-        
Figure C94117303013010
      ＝N-
H         
Figure C94117303013011
                 -(CH2)3-        
Figure C94117303013012
      ＝N-
H        S-CH2-COOC5H11-n               -(CH2)3-        
Figure C94117303013013
      ＝N-表1(续)
R1      R2                              A              E           G
H        
Figure C9411730301311
                 -(CH2)3-           ＝N-
H        
Figure C9411730301313
            -(CH2)3-    
Figure C9411730301314
      ＝N-
H        O-CH2CH2-OCH(CH2F)2       -(CH2)3-    
Figure C9411730301315
      ＝N-
H        S-CH(CH3)2                  -(CH2)3-    
Figure C9411730301316
      ＝N-
H        O-CH2-CCl＝CH2              -(CH2)3-            ＝N-
H        
Figure C9411730301318
                 -(CH2)3-            ＝N-
H        O-CH2CN                      -(CH2)3-            ＝N-
H        O-CH2COOC2H4-OCH3         -(CH2)3-         ＝N-表1(续)
R1      R2                            A            E            G
H        O-CH2-COO-CH(CH3)COOC2H5   -(CH2)3-   
Figure C9411730301321
    ＝N-
H        OCH2-COOCH2-COOC2H5        -(CH2)3-        ＝N-
H        O-CHF2                        -(CH2)3-        ＝N-
H        O-CH2CH2-OCH2CF3           -(CH2)3-   
Figure C9411730301324
    ＝N-
H        NHCH3                         -(CH2)3-        ＝N-
H        NHC2H5                       -(CH2)3-        ＝N-
H        N(CH3)2                      -(CH2)3-   
Figure C9411730301327
    ＝N-
H        NH-CH2-COOC2H5              -(CH2)3-   
Figure C9411730301328
    ＝N-表1(续)
R1       R2                       A              E            G
H         
Figure C9411730301331
              -(CH2)3-            ＝N-
H                           -(CH2)3-     
Figure C9411730301334
      ＝N-
H         ZNH-SO2CH3             -(CH2)3-            ＝N-
H         NH-SO2C2H5            -(CH2)3-     
Figure C9411730301336
      ＝N-
H         NH-SO2C3H7-n          -(CH2)3-     
Figure C9411730301337
      ＝N-
H         NH-SO2C3H7-i          -(CH2)3-     
Figure C9411730301338
      ＝N-
H         NH-SO2C4H9-n          -(CH2)3-     
Figure C9411730301339
      ＝N-
H         NH-SO2C8H17-n         -(CH2)3-     
Figure C94117303013310
      ＝N-表1(续)
R1      R2                       A               E             G
H        NH-COCH3                 -(CH2)3-             ＝N-
H        NH-COC2H5               -(CH2)3-             ＝N-
H        NH-COCF3                 -(CH2)3-      
Figure C9411730301343
      ＝N-
H        N(CH3)-SO2CH3          -(CH2)3-      
Figure C9411730301344
      ＝N-
H        N(CH3)-SO2C2H5        -(CH2)3-      
Figure C9411730301345
      ＝N-
H        N(CH3)-SO2C3H7-n      -(CH2)3-             ＝N-
H        NH-SO2CF3               -(CH2)3-      
Figure C9411730301347
      ＝N-
H        
Figure C9411730301348
             -(CH2)3-             ＝N-表1(续)
R1       R2                         A                E          G
H         NH-SO2-C4F9-n            -(CH2)3-      
Figure C9411730301351
   ＝N-
H         N(CH3)SO2CF3             -(CH2)3-          ＝N-
H                      -(CH2)3-      
Figure C9411730301354
   ＝N-
H         
Figure C9411730301355
          -(CH2)3-          ＝N-
H         
Figure C9411730301357
     -(CH2)3-          ＝N-
Cl          OCH2CF3                 -(CH2)3-      
Figure C9411730301359
   ＝N-表1(续)
R1       R2                          A              E          G
Cl        OCF3                        -(CH2)3-     
Figure C9411730301361
   ＝N-
Cl        OCH2CH(CH3)-OC2H5       -(CH2)3-         ＝N-
Cl        
Figure C9411730301363
               -(CH2)3-     
Figure C9411730301364
   ＝N-
Cl        OCH2-CH＝CH2              -(CH2)3-     
Figure C9411730301365
   ＝N-
C1        OH                          -(CH2)3-     
Figure C9411730301366
    ＝N-表1(续)
R1      R2                   A              E             G
Cl       OCH2-C＝CH           -(CH2)3-     
Figure C9411730301371
      ＝N-
Cl       SCH2C≡CH            -(CH2)3-            ＝N-
Cl       OCH2COOC2H5        -(CH2)3-            ＝N-
Cl       S-C(CH3)3           -(CH2)3-     
Figure C9411730301374
      ＝N-
Cl       OCH2-COOC5H11-n    -(CH2)3-     
Figure C9411730301375
      ＝N-
Cl       OCH(CH3)-COOC2H5   -(CH2)3-            ＝N-表1(续)
R1      R2                     A                E             G
Cl       OCH2CH2-OCH3         -(CH2)3-     
Figure C9411730301381
     ＝N-
Cl       OCH2CH2-OC2H5       -(CH2)3-    
Figure C9411730301382
    ＝N-
Cl       O(CH2CH2O)2-OC2H5  -(CH2)3-     
Figure C9411730301383
     ＝N-
Cl       S-C3H7-n              -(CH2)3-     
Figure C9411730301384
     ＝N-
Cl       S-C2H5                -(CH2)3-           ＝N-
Cl       S-CH3                  -(CH2)3-     
Figure C9411730301386
     ＝N-
Cl       S-CH2COOC2H5         -(CH2)3-     
Figure C9411730301387
     ＝N-
Cl       SCH2CH2-COOC2H5     -(CH2)3-    
Figure C9411730301388
    ＝N-
Cl       C-CH2-C≡C-CH3        -(CH2)3-           ＝N-
Cl       OCH2C＝CH-Cl           -(CH2)3-     
Figure C94117303013810
     ＝N-表1(续)
R1       R2                       A                   E           G
Cl        O-CH(CH3)C≡CH           -(CH2)3-         
Figure C9411730301391
     ＝N-
Cl        OCH(CH3)C≡C-CH3        -(CH2)3-               ＝N-
Cl        O-CH(CH3)CH＝CH2        -(CH2)3-         
Figure C9411730301393
     ＝N-
Cl        OCH2CH＝CH-CH3          -(CH2)3-         
Figure C9411730301394
     ＝N-
Cl        O-CH3                    -(CH2)3-         
Figure C9411730301395
     ＝N-
Cl        O-C2H5                  -(CH2)3-         
Figure C9411730301396
     ＝N-
Cl        O-C3H7-n                -(CH2)3-         
Figure C9411730301397
     ＝N-
Cl        O-C3H7-iso              -(CH2)3-         
Figure C9411730301398
    ＝N-表1(续)
R1   R2                                  A               E         G
Cl    
Figure C9411730301401
                          -(CH2)3-    
Figure C9411730301402
    ＝N-
Cl    
Figure C9411730301403
                          -(CH2)3-    
Figure C9411730301404
    ＝N-
Cl    O-CH(CH2F)2                        -(CH2)3-    
Figure C9411730301405
    ＝N-
Cl    O-CH2-C(CH3)＝CH2                -(CH2)3-    
Figure C9411730301406
    ＝N-
Cl                             -(CH2)3-    
Figure C9411730301408
    ＝N-
Cl    
Figure C9411730301409
                      -(CH2)3-         ＝N-
Cl                          -(CH2)3-    
Figure C94117303014012
    ＝N-表1(续)
R1   R2                                 A                E          G
Cl    
Figure C9411730301411
                       -(CH2)3-          ＝N-
Cl                           -(CH2)3-      
Figure C9411730301414
   ＝N-
Cl    
Figure C9411730301415
                  -(CH2)3-          ＝N-
Cl    S-CH2-COOC5H11-n                -(CH2)3-      
Figure C9411730301417
    ＝N-
Cl    
Figure C9411730301418
                      -(CH2)3-      
Figure C9411730301419
   ＝N-
Cl    
Figure C94117303014110
                      -(CH2)3-          ＝N-
Cl    O-CH2CH2-OCH(CH2F)2             -(CH2)3-      
Figure C94117303014112
   ＝N-表1(续)
R1       R2                          A                E            G
Cl        S-CH(CH3)2                 -(CH2)3-             ＝N-
Cl        O-CH2-CCl＝CH2             -(CH2)3-       
Figure C9411730301422
     ＝N-
Cl        
Figure C9411730301423
                  -(CH2)3-             ＝N-
Cl        O-CH2CN                     -(CH2)3-       
Figure C9411730301425
     ＝N-
Cl        O-CH2COOC2H4-OCH3        -(CH2)3-       
Figure C9411730301426
     ＝N-
Cl        O-CH2-COO-CH(CH3)COOC2H5 -(CH2)3-       
Figure C9411730301427
     ＝N-
Cl        OCH2-COOCH2-COOC2H5      -(CH2)3-       
Figure C9411730301428
     ＝N-
Cl        O-CHF2                      -(CH2)3-       
Figure C9411730301429
     ＝N-
Cl        O-CH2CH2-OCH2CF3         -(CH2)3-       
Figure C94117303014210
     ＝N-表1(续)
R1       R2                     A                  E              G
Cl        NHCH3                  -(CH2)3-         
Figure C9411730301431
       ＝N-
Cl        NHC2H5                -(CH2)3-         
Figure C9411730301432
       ＝N-
Cl        N(CH3)2               -(CH2)3-         
Figure C9411730301433
       ＝N-
Cl        NH-CH2-COOC2H5       -(CH2)3-         
Figure C9411730301434
       ＝N-
Cl        
Figure C9411730301435
           -(CH2)3-         
Figure C9411730301436
       ＝N-
Cl        
Figure C9411730301437
               -(CH2)3-                  ＝N-
Cl        NH-SO2CH3             -(CH2)3-         
Figure C9411730301439
       ＝N-
Cl        NH-SO2C2H5           -(CH2)3-         
Figure C94117303014310
      ＝N-表1(续)
R1        R2                         A                E             G
Cl         NH-SO2C3H7-n             -(CH2)3-              ＝N-
Cl         NH-SO2C3H7-i             -(CH2)3-       
Figure C9411730301442
      ＝N-
Cl         NH-SO2C4H9-n             -(CH2)3-       
Figure C9411730301443
      ＝N-
Cl         NH-SO2C8H17-n            -(CH2)3-       
Figure C9411730301444
      ＝N-
Cl         NH-COCH3                   -(CH2)3-              ＝N-
Cl         NH-COC2H5                 -(CH2)3-       
Figure C9411730301446
      ＝N-
Cl         NH-COCF3                   -(CH2)3-              ＝N-
Cl         N(CH3)-SO2CH3            -(CH2)3-       
Figure C9411730301448
     ＝N-表1(续)
R1        R2                       A                  E               G
Cl         N(CH3)-SO2C2H5        -(CH2)3-         
Figure C9411730301451
      ＝N-
Cl         N(CH3)-SO2C3H7-n      -(CH2)3-         
Figure C9411730301452
    ＝N-
Cl         NH-SO2CF3               -(CH2)3-         
Figure C9411730301453
      ＝N-
Cl                      -(CH2)3-         
Figure C9411730301455
      ＝N-
Cl         NH-SO2-C4F9-n          -(CH2)3-         
Figure C9411730301456
      ＝N-
Cl         N(CH3)SO2CF3           -(CH2)3-         
Figure C9411730301457
      ＝N-
Cl                     -(CH2)3-         
Figure C9411730301459
      ＝N-
Cl         
Figure C94117303014510
        -(CH2)3-         
Figure C94117303014511
     ＝N-表1(续)
R1       R2                            A                       E              G
Cl        
Figure C9411730301461
        -(CH2)3-                       ＝N-
F        O-CH(CH2F)2                   -CH2C(CH3)2-CH2-   
Figure C9411730301463
         ＝N-
F        O-CH2-C(CH3)＝CH2           -CH2C(CH3)2-CH2-   
Figure C9411730301464
         ＝N-
F        
Figure C9411730301465
              -CH2C(CH3)2-CH2-   
Figure C9411730301466
         ＝N-
F        
Figure C9411730301467
                 -CH2C(CH3)2-CH2-   
Figure C9411730301468
        ＝N-
F        
Figure C9411730301469
                   -CH2C(CH3)2-CH2-             ＝N-
F                            -CH2C(CH3)2-CH2-   
Figure C94117303014612
         ＝N-表1(续)
R1      R2                      A                         E            G
F        
Figure C9411730301471
             -CH2C(CH3)2-CH2-     
Figure C9411730301472
      ＝N-
F        
Figure C9411730301473
        -CH2C(CH3)2-CH2-     
Figure C9411730301474
      ＝N-
F        S-CH2-COOC5H11-n    -CH2C(CH3)2-CH2-             ＝N-
F        
Figure C9411730301476
         -CH2C(CH3)2-CH2-     
Figure C9411730301477
       ＝N-
F        
Figure C9411730301478
          -CH2C(CH3)2-CH2-            ＝N-
F        OCH2CH2-OCH(CH2F)2 -CH2C(CH3)2-CH2-            ＝N-
F        S-CH(CH3)2           -CH2C(CH3)2-CH2-     
Figure C94117303014711
      ＝N-
F        O-CH2-CCl＝CH2       -CH2C(CH3)2-CH2-     
Figure C94117303014712
      ＝N-表1(续)
R1       R2                         A                         E          G
F                      -CH2C(CH3)2-CH2-     
Figure C9411730301482
     ＝N-
F        O-CH2CN                     -CH2C(CH3)2-CH2-     
Figure C9411730301483
     ＝N-
F        O-CH2COOC2H4-OCH3       -CH2C(CH3)2-CH2-     
Figure C9411730301484
     ＝N-
F        O-H2-COO-CH(CH3)COOC2H5 -CH2C(CH3)2-CH2-     
Figure C9411730301485
     ＝N-
F        OCH2-COOCH2-COOC2H5     -CH2C(CH3)2-CH2-           ＝N-
F        O-CHF2                     -CH2C(CH3)2-CH2-           ＝N-
F        O-CH2CH2-OCH2CF3        -CH2C(CH3)2-CH2-           ＝N-
F        OCH2CF3                   -CH2C(CH3)2-CH2-     
Figure C9411730301489
     ＝N-表1(续)
R1  R2                     A                         E                G
F    OCF3                   -CH2C(CH3)2-CH2-              ＝N-
F    OCH2CH(CH3)-OC2H5   -CH2C(CH3)2-CH2-     
Figure C9411730301492
       ＝N-
F              -CH2C(CH3)2-CH2-      
Figure C9411730301494
       ＝N-
F    OCH2-CH＝CH2          -CH2C(CH3)2-CH2-      
Figure C9411730301495
       ＝N-
F    OH                      -CH2C(CH3)2-CH2-      
Figure C9411730301496
       ＝N-
F    OCH2-C≡CH             -CH2C(CH3)2-CH2-      
Figure C9411730301497
       ＝N-
F    SCH2C≡CH              -CH2C(CH3)2-CH2-      
Figure C9411730301498
       ＝N-
F    OCH2COOC2H5          -CH2C(CH3)2-CH2-      
Figure C9411730301499
       ＝N-表1(续)
R1  R2                     A                         E             G
F    S-C(CH3)3             -CH2C(CH3)2-CH2-      
Figure C9411730301501
      ＝N-
F    OCH2-COOC5H11-n      -CH2C(CH3)2-CH2-      
Figure C9411730301502
      ＝N-
F    OCH(CH3)-COOC2H5     -CH2C(CH3)2-CH2-      
Figure C9411730301503
      ＝N-
F    OCH2CH2-OCH3         -CH2C(CH3)2-CH2-      
Figure C9411730301504
      ＝N-
F    OCH2CH2-OC2H5       -CH2C(CH3)2-CH2-             ＝N-
F    O(CH2CH2O)2-OC2H5  -CH2C(CH3)2-CH2-      
Figure C9411730301506
      ＝N-
F    S-C3H7-n              -CH2C(CH3)2-CH2-      
Figure C9411730301507
      ＝N-
F    S-C2H5                -CH2C(CH3)2-CH2-             ＝N-表1(续)
R1   R2                   A                        E           G
F    S-CH3                -CH2C(CH3)2-CH2-            ＝N-
F    S-CH2COOC2H5       -CH2C(CH3)2-CH2-     
Figure C9411730301512
      ＝N-
F    SCH2CH2-COOC2H5   -CH2C(CH3)2-CH2-     
Figure C9411730301513
      ＝N-
F    O-CH2-C≡C-CH3      -CH2C(CH3)2-CH2-     
Figure C9411730301514
      ＝N-
F    OCH2-CH＝CH-Cl       -CH2C(CH3)2-CH2-     
Figure C9411730301515
      ＝N-
F    O-CH(CH3)C≡CH       -CH2C(CH3)2-CH2-            ＝N-
F    OCH(CH3)C≡C-CH3    -CH2C(CH3)2-CH2-     
Figure C9411730301517
      ＝N-
F    O-CH(CH3)CH＝CH2    -CH2C(CH3)2-CH2-     
Figure C9411730301518
      ＝N-表1(续)
R1  R2                   A                          E              G
F    OCH2CH＝CH-CH3      -CH2C(CH3)2-CH2-       
Figure C9411730301521
      ＝N-
F    O-CH3                -CH2C(CH3)2-CH2-              ＝N-
F    O-C2H5              -CH2C(CH3)2-CH2-       
Figure C9411730301523
      ＝N-
F    O-C3H7-n            -CH2C(CH3)2-CH2-       
Figure C9411730301524
      ＝N-
F    O-C3H7-iso          -CH2C(CH3)2-CH2-              ＝N-
F    
Figure C9411730301526
           -CH2C(CH3)2-CH2-       
Figure C9411730301527
      ＝N-
F                -CH2C(CH3)2-CH2-              ＝N-
F    NHCH3                -CH2C(CH3)2-CH2-              ＝N-表1(续)
R1  R2                 A                         E               G
F    NHC2H5            -CH2C(CH3)2-CH2-      
Figure C9411730301531
       ＝N-
F    N(CH3)2           -CH2C(CH3)2-CH2-              ＝N-
F    NH-CH2-COOC2H5   -CH2C(CH3)2-CH2-      
Figure C9411730301533
       ＝N-
F    
Figure C9411730301534
             -CH2C(CH3)2-CH2-      
Figure C9411730301535
       ＝N-
F                 -CH2C(CH3)2-CH2-      
Figure C9411730301537
       ＝N-
F    NH-SO2CH3         -CH2C(CH3)2-CH2-      
Figure C9411730301538
       ＝N-
F    NH-SO2C2H5       -CH2C(CH3)2-CH2-      
Figure C9411730301539
       ＝N-
F    NH-SO2C3H7-n     -CH2C(CH3)2-CH2-      
Figure C94117303015310
       ＝N-表1(续)
R1   R2                   A                         E                 G
F    NH-SO2C3H7-i        -CH2C(CH3)2-CH2-               ＝N-
F    NH-SO2C4H9-n        -CH2C(CH3)2-CH2-                ＝N-
F    NH-SO2C8H17-n       -CH2C(CH3)2-CH2-      
Figure C9411730301543
         ＝N-
F    NH-COCH3              -CH2C(CH3)2-CH2-      
Figure C9411730301544
         ＝N-
F    NH-COC2H5            -CH2C(CH3)2-CH2-      
Figure C9411730301545
         ＝N-
F    NH-COCF3              -CH2C(CH3)2-CH2-      
Figure C9411730301546
         ＝N-
F    N(CH3)-SO2CH3       -CH2C(CH3)2-CH2-      
Figure C9411730301547
        ＝N-
F    N(CH3)-SO2C2H5     -CH2C(CH3)2-CH2-      
Figure C9411730301548
        ＝N-表1(续)
R1  R2                     A                      E                 G
F    N(CH3)-SO2C3H7-n    -CH2C(CH3)2-CH2-   
Figure C9411730301551
         ＝N-
F    NH-SO2CF3             -CH2C(CH3)2-CH2-             ＝N-
F    
Figure C9411730301553
        -CH2C(CH3)2-CH2-   
Figure C9411730301554
         ＝N-
F    NH-SO2-C4F9-n        -CH2C(CH3)2-CH2-   
Figure C9411730301555
         ＝N-
F    N(CH3)SO2CF3         -CH2C(CH3)2-CH2-   
Figure C9411730301556
         ＝N-
F    
Figure C9411730301557
       -CH2C(CH3)2-CH2-   
Figure C9411730301558
         ＝N-
F    
Figure C9411730301559
       -CH2C(CH3)2-CH2-            ＝N-表1(续)
R1  R2                      A                       E                G
F    
Figure C9411730301561
   -CH2C(CH3)2-CH2-    
Figure C9411730301562
        ＝N-
H    OCH2CF3                -CH2C(CH3)2-CH2-    
Figure C9411730301563
        ＝N-
H    OCF3                    -CH2C(CH3)2-CH2-    
Figure C9411730301564
        ＝N-
H    OCH2CH(CH3)-OC2H5   -CH2C(CH3)2-CH2-    
Figure C9411730301565
        ＝N-
H    
Figure C9411730301566
             -CH2C(CH3)2-CH2-    
Figure C9411730301567
        ＝N-
H    OCH2-CH＝CH2           -CH2C(CH3)2-CH2-    
Figure C9411730301568
        ＝N-
H    OH                       -CH2C(CH3)2-CH2-             ＝N-
H    OCH2-C≡CH              -CH2C(CH3)2-CH2-    
Figure C94117303015610
        ＝N-表1(续)
R1   R2                    A                        E              G
H    SCH2C≡CH              -CH2C(CH3)2-CH2-     
Figure C9411730301571
       ＝N-
H    OCH2COOC2H5          -CH2C(CH3)2-CH2-     
Figure C9411730301572
       ＝N-
H    S-C(CH3)3             -CH2C(CH3)2-CH2-     
Figure C9411730301573
       ＝N-
H    OCH2-COOC5H11-n      -CH2C(CH3)2-CH2-     
Figure C9411730301574
       ＝N-
H    OCH(CH3)-COOC2H5     -CH2C(CH3)2-CH2-     
Figure C9411730301575
       ＝N-
H    OCH2CH2-OCH3         -CH2C(CH3)2-CH2-     
Figure C9411730301576
       ＝N-
H    OCH2CH2-OC2H5       -CH2C(CH3)2-CH2-             ＝N-
H    O(CH2CH2O)2-OC2H5  -CH2C(CH3)2-CH2-     
Figure C9411730301578
       ＝N-表1(续)
R1   R2                   A                          E                G
H    S-C3H7-n             -CH2C(CH3)2-CH2-       
Figure C9411730301581
         ＝N-
H    S-C2H5               -CH2C(CH3)2-CH2-                 ＝N-
H    S-CH3                 -CH2C(CH3)2-CH2-       
Figure C9411730301583
         ＝N-
H    S-CH2COOC2H5        -CH2C(CH3)2-CH2-                 ＝N-
H    SCH2CH2-COOC2H5    -CH2C(CH3)2-CH2-                 ＝N-
H    O-CH2-C≡CH3         -CH2C(CH3)2-CH2-                 ＝N-
H    OCH2-CH＝CH-Cl        -CH2C(CH3)2-CH2-       
Figure C9411730301587
         ＝N-
H    O-CH(CH3)C≡CH        -CH2C(CH3)2-CH2-       
Figure C9411730301588
         ＝N-表1(续)
R1   R2                     A                            E              G
H     OCH(CH3)C≡C-CH3     -CH2C(CH3)2-CH2-        
Figure C9411730301591
        ＝N-
H     O-CH(CH3)CH＝CH2     -CH2C(CH3)2-CH2-        
Figure C9411730301592
        ＝N-
H     OCH2CH＝CH-CH3       -CH2C(CH3)2-CH2-                 ＝N-
H     O-CH3                 -CH2C(CH3)2-CH2-        
Figure C9411730301594
        ＝N-
H     O-C2H5               -CH2C(CH3)2-CH2-        
Figure C9411730301595
        ＝N-
H     O-C3H7-n             -CH2C(CH3)2-CH2-        
Figure C9411730301596
        ＝N-
H     O-C3H7-iso           -CH2C(CH3)2-CH2-        
Figure C9411730301597
        ＝N-
H              -CH2C(CH3)2-CH2-        
Figure C9411730301599
        ＝N-
H     
Figure C94117303015910
            -CH2C(CH3)2-CH2-                 ＝N-
H    O-CH(CH2F)2           -CH2C(CH3)2-CH2-                ＝N-表1(续)
R1   R2                             A                          E                G
H     O-CH2-C(CH3)-CH2           -CH2C(CH3)2-CH2-                ＝N-
H                        -CH2C(CH3)2-CH2-                ＝N-
H     
Figure C9411730301604
              -CH2C(CH3)2-CH2-       
Figure C9411730301605
        ＝N-
H                        -CH2C(CH3)2-CH2-                ＝N-
H     
Figure C9411730301608
                  -CH2C(CH3)2-CH2-       
Figure C9411730301609
        ＝N-
H     
Figure C94117303016010
                  -CH2C(CH3)2-CH2-                 ＝N-
H     
Figure C94117303016012
             -CH2C(CH3)2-CH2-                 ＝N-
H    S-CH2-COOC5H11-n           -CH2C(CH3)2-CH2-       
Figure C94117303016014
         ＝N-表1(续)
R1  R2                          A                        E             G
H    
Figure C9411730301611
            -CH2C(CH3)2-CH2-     
Figure C9411730301612
        ＝N-
H                 -CH2C(CH3)2-CH2-     
Figure C9411730301614
        ＝N-
H    O-CH2CH2-OCH(CH2F)2   -CH2C(CH3)2-CH2-     
Figure C9411730301615
         ＝N-
H    S-CH(CH3)2              -CH2C(CH3)2-CH2-     
Figure C9411730301616
         ＝N-
H    O-CH2-CCl＝CH2          -CH2C(CH3)2-CH2-     
Figure C9411730301617
         ＝N-
H    
Figure C9411730301618
               -CH2C(CH3)2-CH2-     
Figure C9411730301619
         ＝N-
H    O-CH2CN                  -CH2C(CH3)2-CH2-     
Figure C94117303016110
         ＝N-
H    O-CH2COOC2H4-OCH3     -CH2C(CH3)2-CH2-     
Figure C94117303016111
        ＝N-表1(续)
R1  R2                                A                        E          G
H    O-CH2-COO-CH(CH3)COOC2H5  -CH2C(CH3)2-CH2-            ＝N-
H    OCH2-COOCH2-COOC2H5      -CH2C(CH3)2-CH2-             ＝N-
H    O-CF2                       -CH2C(CH3)2-CH2-     
Figure C9411730301623
       ＝N-
H    OCH2CH2-OCH2CF3          -CH2C(CH3)2-CH2-     
Figure C9411730301624
      ＝N-
H    NHCH3                       -CH2C(CH3)2-CH2-     
Figure C9411730301625
       ＝N-
H    NHC2H5                     -CH2C(CH3)2-CH2-     
Figure C9411730301626
       ＝N-
H    N(CH3)2                   -CH2C(CH3)2-CH2-     
Figure C9411730301627
        ＝N-
H    NH-CH2-COOC2H5           -CH2C(CH3)2-CH2-     
Figure C9411730301628
       ＝N-表1(续)
R1   R2                      A                     E               G
H     
Figure C9411730301631
          -CH2C(CH3)2-CH2-   
Figure C9411730301632
           ＝N-
H     
Figure C9411730301633
             -CH2C(CH3)2-CH2-   
Figure C9411730301634
           ＝N-
H     NH-SO2CH3          -CH2C(CH3)2-CH2-   
Figure C9411730301635
           ＝N-
H     NH-SO2C2H5        -CH2C(CH3)2-CH2-   
Figure C9411730301636
           ＝N-
H     NH-SO2C3H7-n      -CH2C(CH3)2-CH2-   
Figure C9411730301637
           ＝N-
H     NH-SO2C3H7-i      -CH2C(CH3)2-CH2-               ＝N-
H     NH-SO2C4H9-n      -CH2C(CH3)2-CH2-               ＝N-
H     NH-SO2C8H17-n     -CH2C(CH3)2-CH2-                ＝N-表1(续)
R1   R2                  A                          E                G
H     NH-COCH3            -CH2C(CH3)2-CH2-                ＝N-
H     NH-COC2H5          -CH2C(CH3)2-CH2-                ＝N-
H     NH-COCF3            -CH2C(CH3)2-CH2-       
Figure C9411730301643
        ＝N-
H     N(CH3)-SO2CH3     -CH2C(CH3)2-CH2-       
Figure C9411730301644
        ＝N-
H     N(CH3)-SO2C2H5   -CH2C(CH3)2-CH2-       
Figure C9411730301645
        ＝N-
H     N(CH3)-SO2C3H7-n -CH2C(CH3)2-CH2-       
Figure C9411730301646
        ＝N-
H     NH-SO2CF3           -CH2C(CH3)2-CH2-       
Figure C9411730301647
        ＝N-
H               -CH2C(CH3)2-CH2-       
Figure C9411730301649
        ＝N-表1(续)
R1   R2                          A                          E               G
H     NH-SO2-C4F9-n         -CH2C(CH3)2-CH2-                  ＝N-
H     N(CH3)SO2CF3          -CH2C(CH3)2-CH2-       
Figure C9411730301652
          ＝N-
H     
Figure C9411730301653
          -CH2C(CH3)2-CH2-       
Figure C9411730301654
          ＝N-
H     
Figure C9411730301655
        -CH2C(CH3)2-CH2-       
Figure C9411730301656
          ＝N-
H     
Figure C9411730301657
  -CH2C(CH3)2-CH2-       
Figure C9411730301658
          ＝N-
Cl    OCH2CF3                -CH2C(CH3)2-CH2-       
Figure C9411730301659
           ＝N-
Cl    OCF3                    -CH2C(CH3)2-CH2-       
Figure C94117303016510
           ＝N-表1(续)
R1   R2                        A                             E             G
Cl    OCH2CH(CH3)-OC2H5    -CH2C(CH3)2-CH2-        
Figure C9411730301661
        ＝N-
Cl            -CH2C(CH3)2-CH2-        
Figure C9411730301663
        ＝N-
Cl    OCH2-CH＝CH2           -CH2C(CH3)2-CH2-        
Figure C9411730301664
        ＝N-
Cl    OH                       -CH2C(CH3)2-CH2-        
Figure C9411730301665
        ＝N-
Cl    OCH2-C≡CH              -CH2C(CH3)2-CH2-        
Figure C9411730301666
        ＝N-
Cl    SCH2C≡CH               -CH2C(CH3)2-CH2-        
Figure C9411730301667
        ＝N-
Cl    OCH2COOC2H5           -CH2C(CH3)2-CH2-                 ＝N-
Cl    S-C(CH3)3              -CH2C(CH3)2-CH2-        
Figure C9411730301669
        ＝N-表1(续)
R1   R2                       A                         E               G
Cl    OCH2-COOC5H11-n        -CH2C(CH3)2-CH2-      
Figure C9411730301671
       ＝N-
Cl    OCH(CH3)-COOC2H5       -CH2C(CH3)2-CH2-              ＝N-
Cl    OCH2CH2-OCH3           -CH2C(CH3)2-CH2-      
Figure C9411730301673
       ＝N-
Cl    OCH2CH2-OC2H5         -CH2C(CH3)2-CH2-      
Figure C9411730301674
       ＝N-
Cl    O(CH2CH2O)2-OC2H5    -CH2C(CH3)2-CH2-      
Figure C9411730301675
       ＝N-
Cl    S-C3H7-n                -CH2C(CH3)2-CH2-      
Figure C9411730301676
       ＝N-
Cl    S-C2H5                  -CH2C(CH3)2-CH2-      
Figure C9411730301677
       ＝N-
Cl    S-CH3                    -CH2C(CH3)2-CH2-      
Figure C9411730301678
       ＝N-表1(续)
R1   R2                      A                          E             G
Cl    S-CH2COOC2H5          -CH2C(CH3)2-CH2-              ＝N-
Cl    SCH2CH2-COOC2H5      -CH2C(CH3)2-CH2-       
Figure C9411730301682
      ＝N-
Cl    O-CH2-C＝C-CH3         -CH2C(CH3)2-CH2-       
Figure C9411730301683
      ＝N-
Cl    OCH2-CH＝CH-Cl          -CH2C(CH3)2-CH2-              ＝N-
Cl    O-CH(CH3)C≡CH          -CH2C(CH3)2-CH2-       
Figure C9411730301685
      ＝N-
Cl    OCH(CH3)C≡C-CH3       -CH2C(CH3)2-CH2-       
Figure C9411730301686
      ＝N-
Cl    O-CH(CH3)CH＝CH2       -CH2C(CH3)2-CH2-       
Figure C9411730301687
      ＝N-
Cl    OCH2CH＝CH-CH3         -CH2C(CH3)2-CH2-       
Figure C9411730301688
      ＝N-表1(续)
R1       R2                A                           E             G
Cl        O-CH3             -CH2C(CH3)2-CH2-      
Figure C9411730301691
      ＝N-
Cl        O-C2H5           -CH2C(CH3)2-CH2-      
Figure C9411730301692
      ＝N-
Cl        O-C3H7-n         -CH2C(CH3)2-CH2-      
Figure C9411730301693
      ＝N-
Cl        O-C3H7-iso       -CH2C(CH3)2-CH2-             ＝N-
Cl        
Figure C9411730301695
        -CH2C(CH3)2-CH2-             ＝N-
Cl        
Figure C9411730301697
         -CH2C(CH3)2-CH2-      
Figure C9411730301698
      ＝N-
Cl        O-CH(CH2F)2      -CH2C(CH3)2-CH2-      
Figure C9411730301699
     ＝N-表1(续)
R1   R2                             A                           E               G
Cl    O-CH2-C(CH3)-CH2            -CH2C(CH3)2-CH2-        
Figure C9411730301701
        ＝N-
Cl                        -CH2C(CH3)2-CH2-                 ＝N-
Cl    
Figure C9411730301704
                  -CH2C(CH3)2-CH2-        
Figure C9411730301705
        ＝N-
Cl    
Figure C9411730301706
                  -CH2C(CH3)2-CH2-        
Figure C9411730301707
       ＝N-
Cl    
Figure C9411730301708
                    -CH2C(CH3)2-CH2-                 ＝N-
Cl    
Figure C94117303017010
                  -CH2C(CH3)2-CH2-        
Figure C94117303017011
        ＝N-
Cl    
Figure C94117303017012
                -CH2C(CH3)2-CH2-        
Figure C94117303017013
        ＝N-
Cl    S-CH2-COOC5H11-n             -CH2C(CH3)2-CH2-                 ＝N-表1(续)
R1   R2                       A                       E                G
Cl                  -CH2C(CH3)2-CH2-   
Figure C9411730301712
        ＝N-
Cl    
Figure C9411730301713
             -CH2C(CH3)2-CH2-   
Figure C9411730301714
        ＝N-
Cl    O-CH2CH2-OCH(CH2F)2   -CH2C(CH3)2-CH2-   
Figure C9411730301715
        ＝N-
Cl    S-CH(CH3)2              -CH2C(CH3)2-CH2-    
Figure C9411730301716
        ＝N-
Cl    O-CH2-CCl＝CH2          -CH2C(CH3)2-CH2-             ＝N-
Cl    
Figure C9411730301718
               -CH2C(CH3)2-CH2-             ＝N-
Cl    O-CH2CN                  -CH2C(CH3)2-CH2-    
Figure C94117303017110
        ＝N-
Cl    O-CH2COOC2H4-OCH3     -CH2C(CH3)2-CH2-    
Figure C94117303017111
       ＝N-表1(续)
R1   R2                          A                             E              G
Cl    O-CH2-COO-CH(CH3)COOC2H5 -CH2C(CH3)2-CH2-        
Figure C9411730301721
       ＝N-
Cl    OCH2-COOCH2-COOC2H5      -CH2C(CH3)2-CH2-                ＝N-
Cl    O-CHF2                      -CH2C(CH3)2-CH2-        
Figure C9411730301723
        ＝N-
Cl    O-CH2CH2-OCH2CF3         -CH2C(CH3)2-CH2-        
Figure C9411730301724
        ＝N-
Cl    NHCH3                       -CH2C(CH3)2-CH2-        
Figure C9411730301725
        ＝N-
Cl    NHC2H5                     -CH2C(CH3)2-CH2-                 ＝N-
Cl    N(CH3)2                    -CH2C(CH3)2-CH2-        
Figure C9411730301727
        ＝N-表1(续)
R1   R2                  A                           E                  G
Cl    NH-CH2-COOC2H5    -CH2C(CH3)2-CH2-                   ＝N-
Cl    
Figure C9411730301732
       -CH2C(CH3)2-CH2-        
Figure C9411730301733
          ＝N-
Cl    
Figure C9411730301734
             -CH2C(CH3)2-CH2-        
Figure C9411730301735
          ＝N-
Cl    NH-SO2CH3          -CH2C(CH3)2-CH2-                   ＝N-
Cl    NH-SO2C2H5        -CH2C(CH3)2-CH2-        
Figure C9411730301737
          ＝N-
Cl    NH-SO2C3H7-n      -CH2C(CH3)2-CH2-        
Figure C9411730301738
          ＝N-
Cl    NH-SO2C3H7-i      -CH2C(CH3)2-CH2-                   ＝N-
Cl    NH-SO2C4H9-n      -CH2C(CH3)2-CH2-                   ＝N-
Cl    NH-SO2C8H17-n     -CH2C(CH3)2-CH2-                   ＝N-表1(续)
R1   R2                  A                            E               G
Cl    NH-COCH3            -CH2C(CH3)2-CH2-       
Figure C9411730301741
          ＝N-
Cl    NH-COC2H5          -CH2C(CH3)2-CH2-       
Figure C9411730301742
          ＝N-
Cl    NH-COCF3            -CH2C(CH3)2-CH2-       
Figure C9411730301743
          ＝N-
Cl    N(CH3)-SO2CH3     -CH2C(CH3)2-CH2-       
Figure C9411730301744
          ＝N-
Cl    N(CH3)-SO2C2H5   -CH2C(CH3)2-CH2-       
Figure C9411730301745
          ＝N-
Cl    N(CH3)-SO2C3H7-n -CH2C(CH3)2-CH2-       
Figure C9411730301746
          ＝N-
Cl    NH-SO2CF3          -CH2C(CH3)2-CH2-       
Figure C9411730301747
          ＝N-
Cl    
Figure C9411730301748
         -CH2C(CH3)2-CH2-       
Figure C9411730301749
          ＝N-表1(续)
R1   R2                               A                          E             G
Cl    N-SO2-C4F9-n                -CH2C(CH3)2-CH2-        
Figure C9411730301751
        ＝N-
Cl    N(CH3)SO2CF3                -CH2C(CH3)2-CH2-                 ＝N-
Cl    
Figure C9411730301753
                -CH2C(CH3)2-CH2-        
Figure C9411730301754
        ＝N-
Cl                   -CH2C(CH3)2-CH2-                 ＝N-
Cl    
Figure C9411730301757
       -CH2C(CH3)2-CH2-        
Figure C9411730301758
        ＝N-
F    O-CH(CH2F)2                    -(CH2)5-                  
Figure C9411730301759
        ＝N-
F    O-CH2-C(CH3)＝CH2            -(CH2)5-                  
Figure C94117303017510
        ＝N-
F                     -(CH2)5-                           ＝N-表1(续)
R1   R2                              A              E           G
F                       -(CH2)5-     
Figure C9411730301762
     ＝N-
F     
Figure C9411730301763
                   -(CH2)5-     
Figure C9411730301764
      ＝N-
F                         -(CH2)5-     
Figure C9411730301766
      ＝N-
F     
Figure C9411730301767
               -(CH2)5-            ＝N-
F     
Figure C9411730301769
           -(CH2)5-     
Figure C94117303017610
     ＝N-
F     S-CH2-COOC5H11-n           -(CH2)5-     
Figure C94117303017611
      ＝N-
F                     -(CH2)5-     
Figure C94117303017613
      ＝N-表1(续)
R1      R2                            A              E           G
F                         -(CH2)5-     
Figure C9411730301772
      ＝N-
F        O-CH2CH2-OCH(CH2F)2       -(CH2)5-     
Figure C9411730301773
      ＝N-
F        S-CH(CH3)2                  -(CH2)5-     
Figure C9411730301774
      ＝N-
F        O-CH2-CCl＝CH2              -(CH2)5-            ＝N-
F        
Figure C9411730301776
                   -(CH2)5-     
Figure C9411730301777
      ＝N-
F        O-CH2CN                      -(CH2)5-     
Figure C9411730301778
      ＝N-
F        O-CH2COOC2H4-OCH3         -(CH2)5-            ＝N-
F        O-CH2-COO-CH(CH3)COOC2H5  -(CH2)5-     
Figure C94117303017710
     ＝N-表1(续)
R1      R2                            A                E             G
F        OCH2-COOCH2-COOC2H5      -(CH2)5-               ＝N-
F        O-CHF2                      -(CH2)5-       
Figure C9411730301782
       ＝N-
F        O-CH2CH2-OCH2CF3         -(CH2)5-              ＝N-
F        OCH2CF3                    -(CH2)5-       
Figure C9411730301784
       ＝N-
F        OCF3                        -(CH2)5-       
Figure C9411730301785
       ＝N-
F        OCH2CH(CH3)-OC2H5        -(CH2)5-       
Figure C9411730301786
      ＝N-
F                         -(CH2)5-               ＝N-
F        OCH2-CH＝CH2               -(CH2)5-      
Figure C9411730301789
      ＝N-表1(续)
R1      R2                      A                E               G
F        OH                       -(CH2)5-       
Figure C9411730301791
      ＝N-
F        OCH2-C≡CH              -(CH2)5-              ＝N-
F        SCH2C≡CH               -(CH2)5-       
Figure C9411730301793
      ＝N-
F        OCH2COOC2H5           -(CH2)5-       
Figure C9411730301794
      ＝N-
F        S-C(CH3)3              -(CH2)5-       
Figure C9411730301795
      ＝N-
F        OCH2-COOC5H11-n       -(CH2)5-       
Figure C9411730301796
      ＝N-
F        OCH(CH3)-COOC2H5      -(CH2)5-       
Figure C9411730301797
      ＝N-
F        OCH2CH2-OCH3          -(CH2)5-              ＝N-表1(续)
R1       R2                        A                E            G
F        OCH2CH2-OC2H5           -(CH2)5-     
Figure C9411730301801
      ＝N-
F        O(CH2CH2O)2-OC2H5      -(CH2)5-     
Figure C9411730301802
      ＝N-
F        S-C3H7-n                  -(CH2)5-     
Figure C9411730301803
      ＝N-
F        S-C2H5                    -(CH2)5-     
Figure C9411730301804
      ＝N-
F        S-CH3                      -(CH2)5-     
Figure C9411730301805
      ＝N-
F        S-CH2COOC2H5             -(CH2)5-     
Figure C9411730301806
      ＝N-
F        SCH2CH2-COOC2H5         -(CH2)5-            ＝N-
F        O-CH2-C≡C-CH3            -(CH2)5-     
Figure C9411730301808
      ＝N-表1(续)
R1      R2                         A                E               G
F        OCH2-CH＝CH-Cl-Cl          -(CH2)5-       
Figure C9411730301811
       ＝N-
F        O-CH(CH3)C≡CH             -(CH2)5-       
Figure C9411730301812
       ＝N-
F        OCH(CH3)C≡C-CH3          -(CH2)5-       
Figure C9411730301813
       ＝N-
F        O-CH(CH3)CH＝CH2          -(CH2)5-       
Figure C9411730301814
       ＝N-
F        OCH2CH＝CH-CH3            -(CH2)5-       
Figure C9411730301815
       ＝N-
F        O-CH3                      -(CH2)5-       
Figure C9411730301816
       ＝N-
F        O-C2H5                    -(CH2)5-       
Figure C9411730301817
       ＝N-
F        O-C3H7-n                  -(CH2)5-       
Figure C9411730301818
       ＝N-表1(续)
R1      R2                      A                E               G
F        O-C3H7-iso             -(CH2)5-       
Figure C9411730301821
       ＝N-
F                       -(CH2)5-       
Figure C9411730301823
      ＝N-
F        
Figure C9411730301824
           -(CH2)5-       
Figure C9411730301825
      ＝N-
F        NHCH3                   -(CH2)5-       
Figure C9411730301826
       ＝N-
F        NHC2H5                 -(CH2)5-       
Figure C9411730301827
      ＝N-
F        N(CH3)2                -(CH2)5-       
Figure C9411730301828
      ＝N-
F        NH-CH2-COOC2H5        -(CH2)5-              ＝N-
F        
Figure C94117303018210
                 -(CH2)5-       
Figure C94117303018211
      ＝N-表1(续)
R1       R2                        A               E             G
F         
Figure C9411730301831
               -(CH2)5-      
Figure C9411730301832
       ＝N-
F         NH-SO2CH3                -(CH2)5-              ＝N-
F         NH-SO2C2H5              -(CH2)5-      
Figure C9411730301834
       ＝N-
F         NH-SO2C3H7-n            -(CH2)5-      
Figure C9411730301835
       ＝N-
F         NH-SO2C3H7-i            -(CH2)5-      
Figure C9411730301836
       ＝N-
F         NH-SO2C4H9-n            -(CH2)5-              ＝N-
F         NH-SO2C8H17-n           -(CH2)5-              ＝N-
F         NH-COCH3                  -(CH2)5-      
Figure C9411730301839
       ＝N-表1(续)
R1      R2                         A               E             G
F        NH-COC2H5                 -(CH2)5-              ＝N-
F        NH-COCF3                   -(CH2)5-      
Figure C9411730301842
       ＝N-
F        N(CH3)-SO2CH3            -(CH2)5-      
Figure C9411730301843
       ＝N-
F        N(CH3)-SO2C2H5          -(CH2)5-              ＝N-
F        N(CH3)-SO2C3H7-n        -(CH2)5-              ＝N-
F        NH-SO2CF3                 -(CH2)5-      
Figure C9411730301846
       ＝N-
F        
Figure C9411730301847
              -(CH2)5-       
Figure C9411730301848
       ＝N-表1(续)
R1      R2                        A                 E            G
F        NH-SO2-C4F9-n           -(CH2 )5-      
Figure C9411730301851
        ＝N-
F        N(CH3)SO2CF3            -(CH2)5-              ＝N-
F                    -(CH2)5-      
Figure C9411730301854
        ＝N-
F        
Figure C9411730301855
        -(CH2)5-      
Figure C9411730301856
        ＝N-
F            -(CH2)5-      
Figure C9411730301858
        ＝N-
H        OCH2CF3                  -(CH2)5-      
Figure C9411730301859
        ＝N-
H        OCF3                      -(CH2)5-      
Figure C94117303018510
        ＝N-
H        OCH2CH(CH3)-OC2H5      -(CH2)5-              ＝N-表1(续)
R1       R2                      A             E            G
H         
Figure C9411730301861
            -(CH2)5-   
Figure C9411730301862
       ＝N-
H        OCH2-CH＝CH2            -(CH2)5-   
Figure C9411730301863
       ＝N-
H        OH                        -(CH2)5-   
Figure C9411730301864
       ＝N-
H        OCH2-C≡CH               -(CH2)5-   
Figure C9411730301865
       ＝N-
H        SCH2C≡CH                -(CH2)5-           ＝N-
H        OCH2COOC2H5            -(CH2)5-   
Figure C9411730301867
       ＝N-
H        S-C(CH3)3               -(CH2)5-   
Figure C9411730301868
       ＝N-
H        OCH2-COOC5H11-n        -(CH2)5-   
Figure C9411730301869
       ＝N-表1(续)
R1      R2                        A               E             G
H        OCH(CH3)-COOC2H5        -(CH2)5-    
Figure C9411730301871
      ＝N-
H        OCH2CH2-OCH3            -(CH2)5-    
Figure C9411730301872
      ＝N-
H        OCH2CH2-OC2H5          -(CH2)5-    
Figure C9411730301873
      ＝N-
H        O(CH2CH2O)2-OC2H5     -(CH2)5-    
Figure C9411730301874
      ＝N-
H        S-C3H7-n                 -(CH2)5-           ＝N-
H        S-C2H5                   -(CH2)5-    
Figure C9411730301876
      ＝N-
H        S-CH3                     -(CH2)5-           ＝N-
H        S-CH2COOC2H5            -(CH2)5-    
Figure C9411730301878
     ＝N-表1(续)
R1       R2                      A              E              G
H         SCH2CH2-COOC2H5      -(CH2)5-     
Figure C9411730301881
      ＝N-
H         O-CH2-C≡C-CH3         -(CH2)5-     
Figure C9411730301882
      ＝N-
H         OCH2-CH＝CH-Cl          -(CH2)5-     
Figure C9411730301883
      ＝N-
H         O-CH(CH3)C≡H           -(CH2)5-            ＝N-
H         OCH(CH3)C≡C-CH3       -(CH2)5-     
Figure C9411730301885
      ＝N-
H         O-CH(CH3)CH＝CH2       -(CH2)5-     
Figure C9411730301886
      ＝N-
H         OCH2CH＝CH-CH3         -(CH2)5-            ＝N-
H         O-CH3                   -(CH2)5-           ＝N-表1(续)
R1      R2                     A               E             G
H        O-C2H5                -(CH2)5-      
Figure C9411730301891
      ＝N-
H        O-C3H7-n              -(CH2)5-      
Figure C9411730301892
      ＝N-
H        O-C3H7-iso            -(CH2)5-      
Figure C9411730301893
      ＝N-
H                  -(CH2)5-      
Figure C9411730301895
      ＝N-
H        
Figure C9411730301896
             -(CH2)5-      
Figure C9411730301897
      ＝N-
H        O-CH(CH2F)2           -(CH2)5-      
Figure C9411730301898
      ＝N-
H        O-CH2-C(CH3)＝CH2    -(CH2)5-      
Figure C9411730301899
      ＝N-表1(续)
R1       R2                             A                E             G
H         
Figure C9411730301901
                   -(CH2)5-              ＝N-
H         
Figure C9411730301903
                  -(CH2)5-       
Figure C9411730301904
      ＝N-
H         
Figure C9411730301905
                    -(CH2)5-       
Figure C9411730301906
       ＝N-
H         
Figure C9411730301907
                  -(CH2)5-       
Figure C9411730301908
       ＝N-
H         
Figure C9411730301909
                    -(CH2)5-               ＝N-
H         
Figure C94117303019011
               -(CH2)5-               ＝N-
H         S-CH2-COOC5H11-n            -(CH2)5-       
Figure C94117303019013
       ＝N-
H                         -(CH2)5-       
Figure C94117303019015
         ＝N-表1(续)
R1      R2                           A               E              G
H        
Figure C9411730301911
               -(CH2)5-      
Figure C9411730301912
      ＝N-
H        O-CH2CH2-OCH(CH2F)2       -(CH2)5-      
Figure C9411730301913
      ＝N-
H        S-CH(CH3)2                  -(CH2)5-      
Figure C9411730301914
      ＝N-
H        O-CH2-CCl＝CH2              -(CH2)5-      
Figure C9411730301915
      ＝N-
H        
Figure C9411730301916
                  -(CH2)5-              ＝N-
H        O-CH2CN                      -(CH2)5-              ＝N-
H        O-CH2COOC2H4-OCH3         -(CH2)5-      
Figure C9411730301919
      ＝N-
H        O-CH2-COO-CH(CH3)COOC2H5  -(CH2)5-             ＝N-
H        OCH2-COOCH2-COOC2H5       -(CH2)5-      
Figure C94117303019111
      ＝N-
H        O-CHF2                       -(CH2)5-      
Figure C94117303019112
       ＝N-表1(续)
R1      R2                      A                E              G
H        O-CH2CH2-OCH2CF3     -(CH2)5-       
Figure C9411730301921
        ＝N-
H        NHCH3                   -(CH2)5-       
Figure C9411730301922
        ＝N-
H        NHC2H5                 -(CH2)5-       
Figure C9411730301923
        ＝N-
H        N(CH3)2                -(CH2)5-                ＝N-
H        NH-CH2-COOC2H5        -(CH2)5-       
Figure C9411730301925
        ＝N-
H        
Figure C9411730301926
                 -(CH2)5-       
Figure C9411730301927
        ＝N-
H        
Figure C9411730301928
                 -(CH2)5-       
Figure C9411730301929
        ＝N-
H        NH-SO2CH3              -(CH2)5-       
Figure C94117303019210
       ＝N-表1(续)
R1       R2                        A               E               G
H         NH-SO2C2H5              -(CH2)5-      
Figure C9411730301931
       ＝N-
H         NH-SO2C3H7-n            -(CH2)5-      
Figure C9411730301932
       ＝N-
H         NH-SO2C3H7-i            -(CH2)5-      
Figure C9411730301933
       ＝N-
H         NH-SO2C4H9-n            -(CH2)5-      
Figure C9411730301934
       ＝N-
H         NH-SO2C8H17-n           -(CH2)5-      
Figure C9411730301935
       ＝N-
H         NH-COCH3                  -(CH2)5-      
Figure C9411730301936
       ＝N-
H         NH-COC2H5                -(CH2)5-      
Figure C9411730301937
       ＝N-
H         NH-COCF3                  -(CH2)5-      
Figure C9411730301938
       ＝N-
H         N(CH3)-SO2CH3           -(CH2)5-      
Figure C9411730301939
       ＝N-
H         N(CH3)-SO2C2H5         -(CH2)5-      
Figure C94117303019310
      ＝N-
H         N(CH3)-SO2C3H7-n       -(CH2)5-      
Figure C94117303019311
       ＝N-表1(续)
R1       R2                             A              E           G
H         NH-SO2CF3                  -(CH2)5-     
Figure C9411730301941
       ＝N-
H         
Figure C9411730301942
                 -(CH2)5-     
Figure C9411730301943
       ＝N-
H         NH-SO2-C4F9-n             -(CH2)5-     
Figure C9411730301944
       ＝N-
H         N(CH3)SO2CF3              -(CH2)5-     
Figure C9411730301945
       ＝N-
H         
Figure C9411730301946
            -(CH2)5-     
Figure C9411730301947
       ＝N-
H                     -(CH2)5-     
Figure C9411730301949
       ＝N-
H         
Figure C94117303019410
     -(CH2)5-     
Figure C94117303019411
       ＝N-
Cl        OCH2CF3                    -(CH2)5-             ＝N-
Cl        OCF3                        -(CH2)5-              ＝N-表1(续)
R1       R2                          A                E             G
Cl        OCH2CH(CH3)-OC2H5     -(CH2)5-       
Figure C9411730301951
        ＝N-
Cl        
Figure C9411730301952
              -(CH2)5-       
Figure C9411730301953
        ＝N-
Cl        OCH2-CH＝CH2            -(CH2)5-       
Figure C9411730301954
        ＝N-
Cl        OH                        -(CH2)5-       
Figure C9411730301955
        ＝N-
Cl        OCH2-C≡CH               -(CH2)5-                ＝N-
Cl        SCH2C≡CH                -(CH2)5-       
Figure C9411730301957
        ＝N-
Cl        OCH2COOC2H5            -(CH2)5-       
Figure C9411730301958
        ＝N-
Cl        S-C(CH3)3               -(CH2)5-       
Figure C9411730301959
        ＝N-
Cl        OCH2-COOC5H11-n        -(CH2)5-       
Figure C94117303019510
       ＝N-表1(续)
R1       R2                     A                E            G
Cl        OCH(CH3)-COOC2H5     -(CH2)5-     
Figure C9411730301961
       ＝N-
Cl        OCH2CH2-OCH3         -(CH2)5-             ＝N-
Cl        OCH2CH2-OC2H5       -(CH2)5-             ＝N-
Cl        O(CH2CH2O)2-OC2H5  -(CH2)5-     
Figure C9411730301964
       ＝N-
Cl        S-C3H7-n              -(CH2)5-     
Figure C9411730301965
       ＝N-
Cl        S-C2H5                -(CH2)5-             ＝N-
Cl        S-CH3                  -(CH2)5-     
Figure C9411730301967
       ＝N-
Cl        S-CH2COOC2H5         -(CH2)5-     
Figure C9411730301968
       ＝N-
Cl        SCH2CH2-COOC2H5     -(CH2)5-             ＝N-
Cl        O-CH2-C≡C-CH3        -(CH2)5-     
Figure C94117303019610
       ＝N-
Cl        OCH2-CH＝CH-Cl         -(CH2)5-             ＝N-表1(续)
R1       R2                     A              E              G
Cl        O-CH(CH3)C≡CH         -(CH2)5-     
Figure C9411730301971
      ＝N-
Cl        OCH(CH3)C≡C-CH3      -(CH2)5-            ＝N-
Cl        -OCH(CH3)CH＝H2       -(CH2)5-     
Figure C9411730301973
      ＝N-
Cl        OCH2CH＝CH-CH3        -(CH2)5-     
Figure C9411730301974
      ＝N-
Cl        OCH3                   -(CH2)5-     
Figure C9411730301975
      ＝N-
Cl        O-C2H5                -(CH2)5-     
Figure C9411730301976
      ＝N-
Cl        O-C3H7-n              -(CH2)5-     
Figure C9411730301977
      ＝N-
Cl        O-C3H7-iso            -(CH2)5-            ＝N-
Cl        
Figure C9411730301979
           -(CH2)5-     
Figure C94117303019710
      ＝N-
Cl        
Figure C94117303019711
            -(CH2)5-           ＝N-表1(续)
R1       R2                               A                E              G
Cl        O-CH(CH2F)2                     -(CH2)5-       
Figure C9411730301981
       ＝N-
Cl        O-CH2-C(CH3)＝CH2              -(CH2)5-               ＝N-
Cl        
Figure C9411730301983
                     -(CH2)5-       
Figure C9411730301984
       ＝N-
Cl                          -(CH2)5-       
Figure C9411730301986
       ＝N-
Cl        
Figure C9411730301987
                     -(CH2)5-       
Figure C9411730301988
       ＝N-
Cl        
Figure C9411730301989
                     -(CH2)5-       
Figure C94117303019810
       ＝N-
Cl        
Figure C94117303019811
                     -(CH2)5-                ＝N-表1(续)
R1       R2                       A              E            G
Cl                 -(CH2)5-     
Figure C9411730301992
       ＝N-
Cl        S-CH2-COOC5H11-n       -(CH2)5-     
Figure C9411730301993
       ＝N-
Cl        
Figure C9411730301994
          -(CH2)5-     
Figure C9411730301995
       ＝N-
Cl        
Figure C9411730301996
         -(CH2)5-     
Figure C9411730301997
       ＝N-
Cl        O-CH2CH2-OCH(CH2F)2   -(CH2)5-             ＝N-
Cl        S-CH(CH3)2              -(CH2)5-             ＝N-
Cl        O-CH2-CCl＝CH2          -(CH2)5-     
Figure C94117303019910
       ＝N-
Cl                  -(CH2)5-     
Figure C94117303019912
       ＝N-
Cl        O-CH2CN                  -(CH2)5-     
Figure C94117303019913
      ＝N-表1(续)
R1       R2                           A               E            G
Cl        O-CH2COOC2H4-OCH3         -(CH2)5-      
Figure C9411730302001
      ＝N-
Cl        O-CH2-COO-CH(CH3)COOC2H5  -(CH2)5-      
Figure C9411730302002
      ＝N-
Cl        OCH2-COOCH2-COOC2H5       -(CH2)5-      
Figure C9411730302003
      ＝N-
Cl        O-CHF2                       -(CH2)5-      
Figure C9411730302004
      ＝N-
Cl        O-CH2CH2-OCH2CF3          -(CH2)5-      
Figure C9411730302005
      ＝N-
Cl        NHCH3                        -(CH2)5-             ＝N-
Cl        NHC2H5                      -(CH2)5-      
Figure C9411730302007
      ＝N-
Cl        N(CH3)2                     -(CH2)5-      
Figure C9411730302008
      ＝N-
Cl        NH-CH2-COOC2H5             -(CH2)5-      
Figure C9411730302009
     ＝N-表1(续)
R1        R2                 A                E            G
Cl                       -(CH2)5-     
Figure C9411730302012
      ＝N-
Cl         
Figure C9411730302013
            -(CH2)5-     
Figure C9411730302014
      ＝N-
Cl         NH-SO2CH3         -(CH2)5-     
Figure C9411730302015
      ＝N-
Cl         NH-SO2C2H5       -(CH2)5-            ＝N-
Cl         NH-SO2C3H7-n     -(CH2)5-            ＝N-
Cl         NH-SO2C3H7-i     -(CH2)5-            ＝N-
Cl         NH-SO2C4H9-n     -(CH2)5-            ＝N-
Cl         NH-SO2C8H17-n    -(CH2)5-     
Figure C94117303020110
      ＝N-
Cl         NH-COCH3           -(CH2)5-     
Figure C94117303020111
      ＝N-
Cl         NH-COC2H5         -(CH2)5-     
Figure C94117303020112
      ＝N-表1(续)
R1       R2                     A                E              G
Cl        NH-COCF3               -(CH2)5-       
Figure C9411730302021
       ＝N-
Cl        N(CH3)-SO2CH3        -(CH2)5-               ＝N-
Cl        N(CH3)-SO2C2H5      -(CH2)5-       
Figure C9411730302023
       ＝N-
Cl        N(CH3)-SO2C3H7-n    -(CH2)5-               ＝N-
Cl        NH-SO2CF3             -(CH2)5-               ＝N-
Cl        
Figure C9411730302026
         -(CH2)5-               ＝N-
Cl        NH-SO2-C4F9-n        -(CH2)5-               ＝N-
Cl        N(CH3)SO2CF3         -(CH2)5-       
Figure C9411730302029
       ＝N-
Cl        
Figure C94117303020210
         -(CH2)5-               ＝N-
Cl        
Figure C94117303020212
      -(CH2)5-       
Figure C94117303020213
       ＝N-
Cl        
Figure C94117303020214
 -(CH2)5-              ＝N-
上面所列一般基团的定义或在优选范围内所给的定义既适用于式(I)最终产物又相应地适用于各自制备中所需的起始化合物或中间体。这些基团定义本身也可以任意组合，即在优选化合物的给定范围内组合。
例如，若用1-[N-(4-氰基-2，5-二氟苯基)]-2-亚氨基哌啶硫代甲酰胺作起始化合物，用硫作氧化剂，那么本发明方法(a)的反应过程可用下式路线概括：
Figure C9411730302031
例如，若用1-[N-(4-氰基-2-氯-5-乙氧基苯基)]-四氢-(2H)-哒嗪硫代甲酰胺和光气作起始化合物，那么本发明方法(b)的反应过程可用下式路线概括：
Figure C9411730302032
例如，若用9-(4-氰基-2，5-二氟苯基亚氨基)-8-硫杂-1，6-二氯杂双环[4.3.0]壬-7-酮和甲磺酰胺作起始化合物，那么本发明方法(c)的反应过程可用下式路线概括：
Figure C9411730302041
在本发明方法(a)中用作制备式(I)化合物起始化合物的取代的硫代羰基氨基化合物一般可用式(II)定义。在式(II)中，R1、R2和A优选或特别具有本发明式(I)化合物描述中优选或特别优选的R1、R2和A的定义。
用作起始化合物的式(II)的取代的硫代羰基氨基化合物由文献来说还是未知的，作为新化合物，它们也是本申请的主题。
新的式(II)化合物可用下列方法制备：使通式(VIII)的异硫氰酸氰基芳基酯：
Figure C9411730302042
其中：R1和R2具有上述定义，
与通式(IX)的亚氨基化合物反应，
Figure C9411730302051
其中：A具有上述定义，反应任选在稀释剂例如甲苯存在下在温度为0℃至100℃之间进行(参考制备实施例)。
除异硫氰酸3-氯-4-氰基苯基酯和异硫氰酸3-三氟甲基-4-氰基苯基酯外，用作前体的式(VIII)的异硫氰酸氰基芳基酯由文献来说还是未知的，作为新化合物，它们是本申请的主题。
新的式(VIII)的异硫氰酸氰基芳基酯可用下列方法制备；使相应的通式(X)的氰基芳基胺：
Figure C9411730302052
其中：R1和R2具有上述定义，与硫光气反应，且任选在反应辅助剂如碳酸钙存在下和任选在稀释剂如二氯甲烷和水存在下在温度为0℃至100℃之间进行(参考制备实施例)。
通式(X)的氰基芳基胺是已知的和/或可按本身已知的方法制备(参考EP-224001)。
通式(Xa)的氰基芳基胺：其中：
R1、R4和R5具有上述定义，和
Y代表CO或SO2，由文献来说还是未知的，作为新化合物，它们是本申请的主题。
新的式(Xa)的氰基芳基胺可用下列方法制备：使相应的通式(XI)的卤代芳基胺：
Figure C9411730302062
其中：R1和X1具有上述定义，与通式(XII)的酰胺反应：
R4-NH-Y-R5                            (XII)其中：R4、R5和Y具有上述定义，且任选在酸性接受体如碳酸钾存在下以及任选在稀释剂如N-甲基吡咯烷酮存在下在温度为100℃至200℃之间进行(参考制备实施例)。
另外作为前体的式(IX)的亚氨基化合物是已知的和/或可用本身已知的方法制备(参考Angew.Chem.81(1969)，431-432；loc.cit.Iht.Ed.Engl.8(1969)，457-458；J.Org.Chem.33(1968)，2109-2111)。
本发明的方法(a)可使用氧化剂或脱氢剂来进行。在此情况下，实际上所有常用作氧化或脱氢的有机化学化合物都是合适的。可以提及的实例是氧、硫、过氧化氢、过硫酸钠、硫代硫酸钠、氯、溴和碘。
本发明的方法(a)优选使用稀释剂来进行。所有常规的有机或无机溶剂均适合于用作稀释剂。特别地，它们包括脂族、脂环或芳香的任意卤代的烃，例如汽油、苯、甲苯、二甲苯、氯苯、二氯苯、石油醚、己烷、环己烷、二氯甲烷、氯仿或四氢化碳；醚类，如乙醚，二异丙基醚、二噁烷、四氢呋喃、乙二醇二甲基醚或乙二醇二乙基醚；酮类，如丙酮、丁酮或甲基异丁基酮；腈类，如乙腈、丙腈或苄腈；酰胺类，如N，N-二甲基甲酰胺、N，N-二甲基乙酰胺、N-甲基-N-甲酰苯胺、N-甲基吡咯烷酮或六甲基磷酰三胺；酯类，如乙酸甲酯或乙酸乙酯；亚砜类，如二甲亚砜；或醇类如甲醇、乙醇、正丙醇或异丙醇、正丁醇、异丁醇、仲丁醇或叔丁醇以及水。
本发明的方法(a)任选在合适的反应辅助剂存在下进行。常规的无机或有机碱特别适合用作上述反应辅助剂。这些碱包括例如碱土金属氢氧化物或碱金属氢氧化物(如氢氧化钠、氢氧化钾、氢氧化钙)以及氢氧化铵，碱金属碳酸(氢)盐如碳酸(氢)钠、碳酸(氢)钾或碳酸铵，碱金属乙酸盐或碱土金属乙酸盐(如乙酸钠、乙酸钾、乙酸钙)或乙酸铵；碱金属醇盐，如甲醇钠或钾，乙醇钠或钾，或叔丁醇钠或钾；以及叔胺类，如三甲胺、三乙胺、三丁胺、N，N-二甲基苯胺、吡啶、N-甲基吡啶、4-二甲氨基吡啶、二氮杂双环辛烷(DABCO)、二氮杂双环壬烯(DBN)或二氮杂双环十一碳烯(DBU)。
在实施本发明的方法(a)中，反应温度可在相对宽的范围内变化。一般地，使用温度为0℃至150℃，优选温度为20℃至120℃。
本发明的方法(a)通常在常压下进行。然而也可在高压或低压下进行。
为了实施本发明的方法(a)，在各种情况下所需的起始化合物通常以大约等摩尔或等当量的量使用。然而，在各种情况下也可以相对大过量地使用一种组分。通常，反应在合适的稀释剂中进行，并将反应混合物在各种情况所需的温度下搅拌，直至转化完全。接着按常规方法进行处理。
在本发明方法(b)中用作制备式(I)化合物的起始化合物的取代的硫代羰基氨基化合物一般可用式(III)定义。
在式(III)中，R1、R2和A优选或特别具有本发明式(I)化合物描述中优选或特别优选的R1、R2和A的上述定义。
用作起始化合物的式(III)的取代的硫代羰基氨基化合物由文献来说还是未知的，作为新化合物，它们是本申请的主题。
新的式(III)化合物可用下列方法制备：使通式(XI)的二氮杂环烷烃或二氮杂环烯烃：
Figure C9411730302081
其中：A具有上述定义，与上述通式(VIII)的异硫氰酸氰基芳基酯反应且任选在稀释剂如甲苯存在下在温度为0℃至100℃下进行(参考制备实施例)。
用作前体的式(XI)的二氮杂环烷烃或二氮杂环烯烃是已知的和/或可按本身已知的方法制备(参考：J.Org.Chem.35(1970)，1468-1471，Tetrahedron 31(1975)，165-170)。
本发明的方法(b)优选使用稀释剂来进行。所有常规惰性有机溶剂适合于用作稀释剂。溶剂特别包括脂族、脂环或芳香的任意卤代的烃，例如汽油、苯、甲苯、二甲苯、氯苯、二氯苯、石油醚、己烷、环己烷、二氯甲烷、氯仿或四氯化碳；醚类，如乙醚、二异丙基醚、二噁烷、四氢呋喃、乙二醇二甲基醚或乙二醇二乙基醚；酰胺类，如N，N-二甲基甲酰胺、N，N-二甲基乙酰胺、N-甲基-N-甲酰苯胺、N-甲基吡咯烷酮或六甲基磷酰三胺；酯类，如乙酸甲酯或乙酸乙酯；亚砜类，如二甲亚砜。
在实施本发明的方法(b)时，反应温度可在相对宽的范围内变化。一般地，使用温度为0℃至150℃，优选温度为10℃至100℃。
本发明的方法(b)通常在常压下进行。然而也可在高压或低压下进行。
为了实施本发明的方法(b)，在各种情况下所需的起始化合物通常以大约等摩尔或等当量的量使用。然而，在各种情况下也可以相对大过量地使用一种组分。通常，反应在合适的稀释剂中进行，并将反应混合物在各种情况所需的温度下搅拌，直至转化完全。接着按常规方法进行处理(参考制备实施例)。
在本发明的方法(c)中，用作起始化合物的取代的氰基芳基亚氨基杂环化合物一般可用式(Ia)定义。在式(Ia)中，R1、A、E和G优选或特别具有本发明式(I)化合物描述中优选或特别优选的R1、A、E和G的上述定义，
X1优选代表氟或氯，特别是代表氟。
根据本发明，式(Ia)起始化合物是新化合物；它们可按本发明的方法(a)或(b)制备。
本发明的方法(c)优选使用稀释剂来进行。所有常规有机或无机溶剂均适合于用作稀释剂。这些溶剂特别包括脂族、脂环或芳香的任意卤代的烃，例如汽油、苯、甲苯、二甲苯、氯苯、二氯苯、石油醚、己烷、环己烷、二氯甲烷、氯仿或四氯化碳；醚类，如乙醚、二异丙基醚、二噁烷、四氢呋喃、乙二醇二甲基醚或乙二醇二乙基醚；酮类，如丙酮、丁酮或甲基异丁基酮；腈类，如乙腈、丙腈或苄腈；酰胺类，如N，N-二甲基甲酰胺、N，N-二甲基乙酰胺、N-甲基-N-甲酰苯胺、N-甲基吡咯烷酮或六甲基磷酰三胺；酯类，如乙酸甲酯或乙酸乙酯；亚砜类，如二甲亚砜；或醇类，如甲醇、乙醇、正丙醇、异丙醇、正丁醇、异丁醇、仲丁醇或叔丁醇，以及水。
本发明的方法(c)任选在酸性接受体存在下进行。常规的无机或有机碱特别适合用作上述接受体。这些碱包括例如碱土金属氢氧化物或碱金属氢氧化物(如氢氧化钠、氢氧化钾、氢氧化钙)以及氢氧化铵，碱金属碳酸(氢)盐  (如碳酸(氢)钠、碳酸(氢)钾)或碳酸铵，碱金属乙酸盐或碱土金属乙酸盐(如乙酸钠、乙酸钾、乙酸钙)或乙酸铵，碱金属醇盐，如甲醇钠或钾，乙醇钠或钾，或叔丁醇钠或钾，以及叔胺，如三甲胺、三乙胺、三丁胺、N，N-二甲基苯胺、吡啶、N-甲基哌啶、4-二甲氨基吡啶、二氮杂双环辛烷(DABC0)、二氮杂双环壬烯(DBN)或二氮杂双环十一碳烯(DBU)。
在实施本发明的方法(c)中，反应温度可在相对宽的范围内变化。一般地，使用温度为0℃至150℃，优选温度为10℃至120℃。
本发明的方法(c)通常在常压下进行。然而也可在高压或低压下进行。
为了实施本发明的方法(c)，在各种情况下所需的起始化合物通常以大约等摩尔或等当量的量使用。然而，在各种情况下也可以相对大过量地使用一种组分。通常，反应在合适的稀释剂中进行，并将反应混合物在各种情况所需的温度下搅拌，直至转化完全。接着按常规方法进行处理。
本发明的活性化合物可用作脱叶剂、干燥剂、除阔叶植物剂，特别是可用作除杂草剂。从最广泛的意义上来说，杂草是指生长在人们所不希望它生长的地方的所有植物。本发明的物质是作为广普性的或选择性的除草剂主要取决于所用的量。
本发明的活性化合物可用于例如下列植物：
下列各属的双子叶植物杂草：欧白芥属、独行菜属、拉拉藤属、繁缕属、母菊属、春黄菊属、牛膝菊属、藜属、荨麻属、千里光属、苋属、马齿苋属、苍耳属、旋花属、番薯属、蓼属、田菁属、豚草属、蓟属、飞廉属、苦苣菜属、茄属、蔊菜属、水松叶属、母草属、野芝麻属、婆婆纳属、苘麻属、刺酸模属、曼陀罗属、堇菜属、鼬瓣花属、罂粟属、矢车菊属、车轴草属、毛茛属和蒲公英属。
下列各属的双子叶栽培作用：棉属、大豆属、甜菜属、胡萝卜属、菜豆属、豌豆属、茄属、亚麻属、番薯属、野豌豆属、烟草属、番茄属、落花生属、芸苔属、莴苣属、香瓜属和南瓜属。
下列各属的单子叶植物杂草：稗属、狗尾草属、黍属、马唐属、梯牧草属、早熟禾属、羊茅属、_属、臂形草属、黑麦草属、雀麦属、燕麦属、莎草属、高梁属、冰草属、狗牙根属、雨久花属、飘拂草属、慈姑属、荸荠属、藨草属、雀稗属、鸭嘴草属、尖瓣花属、龙爪茅属、剪股颖属、看麦娘属和风草属(Apera)。
下列各属的单子叶栽培作物：稻属、玉蜀黍属、小麦属、大麦属、燕麦属、黑麦属、高梁属、黍属、甘蔗属、凤梨属、天门冬属和葱属。
然而，本发明的活性化合物的应用决不局限于这些属，它们也可以同样方式扩展到用于其它植物。
依据其浓度的不同，所述化合物适合于完全除灭例如工业场地、铁路轨道、有和没有植树的道路和广场上的杂草，同样，所述化合物可用于除灭多年生栽培作物(例如造林、观赏林、果园、葡萄园、柑橘园、坚果园、香焦种植园、咖啡种植园、茶叶种植园、橡胶种植园、油棕榈种植园、可可种植园、浆果园、蛇麻草田)中的杂草和在草地、草皮、牧场中的杂草，以及选择性除灭一年生栽培作物中的杂草。
本发明的式(I)化合物特别适合于在芽前和芽后处理过程中选择性除灭单子叶栽培作物中的单子叶和双子叶杂草。
可将活性化合物转化为常规制剂，如溶液、乳液、悬浮液、粉剂、泡沫剂、糊剂、颗粒剂、气雾剂、用活性化合物浸渍的天然和合成物质、以及非常细的聚合物胶囊。
这些制剂可用已知方法制备，例如将活性化合物与增量剂混合，增量剂为液体溶剂、加压液化气体和/或固体载体，任选使用表面活性剂，即乳化剂和/或分散剂和/或生泡剂。
当使用水作为增量剂时，例如也可用有机溶剂作辅助溶剂。适合的液体溶剂主要为：芳香烃如二甲苯、甲苯或烷基萘；氯代芳香烃或氯代脂肪烃如氯苯、氯乙烯或二氯甲烷；脂肪烃如环己烷或烷属烃，例如石油馏分、矿物油和植物油；醇类如丁醇或乙二醇，以及其醚类和酯类；酮类，如丙酮、甲基乙基酮、甲基异丁基酮或环己酮；强极性溶剂如二甲基甲酰胺和二甲亚砜，以及水。
合适的固体载体为：例如铵盐和磨碎的天然矿物(如高岭土、粘土、滑石、白垩、石英、硅镁土、蒙脱石或硅藻土)，以及磨碎的合成矿物(如高分散的二氧化硅、氧化铝和硅酸盐)；合适的颗粒固体载体为：例如粉碎并分级的天然矿石(如方解石、大理石、浮石、海泡石和白云石)以及无机和有机粉末的人造颗粒，和有机物颗粒(如锯末、椰子壳、玉米穗轴和烟草杆)；合适的乳化剂和/或生泡剂为：例如非离子和阴离子乳化剂(如聚氧乙烯脂肪酸酯、聚氧乙烯脂肪醇醚，例如烷基芳基聚乙二醇醚、烷基磺酸盐、烷基硫酸盐、芳基磺酸盐以及白蛋白水解产物)；合适的分散剂为：例如木素-亚硫酸盐废液和甲基纤维素。
在制剂中可以使用粘合剂，如羧甲基纤维素和粉状、颗粒状或胶乳状的天然及合成的聚合物(如阿拉伯树胶、聚乙烯醇和聚乙酸乙烯酯)，以及天然的磷脂(如脑磷脂和卵磷脂)和合成磷脂。其他添加剂可以是矿物油和植物油。
可以使用着色剂，如无机颜料(例如氧化铁、二氧化钛和普鲁士蓝)以及有机染料(如茜素染料、偶氮染料和金属酞菁染料)以及痕量营养素(如铁、锰、硼、铜、钴、钼和锌的盐)。
通常，制剂中含有0.1至95％(重量)，优选0.5至90％(重量)的活性化合物。
为防治杂草，本发明的活性化合物本身或其制剂形式也可以作为与已知除草剂的混合物、成品制剂或可能的罐装混合物使用。
用于上述混合物的合适的除草剂是已知的除草剂，例如N-酰苯胺类，如diflufenican和  敌稗；芳基羧酸类如二氯吡啶甲酸毒草畏或毒莠定；芳氧基链烷酸类，如2，4-滴、2，4-滴丁酸、2，4-滴丙酸、fluroxypyr、2甲4氯、2甲4氯丙酸和定草酯；芳氧基苯氧基链烷酸酯类，例如氯甲草(diclofop-methyl)、fenoxaprop-ethyl，fluazifop-butyl，haloxyfop-methyl和quizalofop-ethyl；连氮酮类(azinones)，如氨基氯哒嗪酮(chloridazon)和达草灭；氨基甲酸酯类，如氯苯胺灵、异苯敌草、苯敌草和苯胺灵；乙酰氯苯胺类，如草不绿、灭草胺、去草胺、甲吡唑安(metazachlor)、丙草胺  (metolachlor)、氯苯胺和毒草胺；二硝基苯胺类，如黄草消、胺硝草和氟乐灵；二苯醚类，如氟锁草醚、治草醚、fluoroglycofen、虎威、halosafen、氟草灭(lactofen)和氟硝草醚(oxyfluorfen)；脲类，如绿麦隆、敌草隆、伏草隆、异丙隆、利谷隆和噻唑隆；羟胺类，如枯杀达、clethodim、cycloxydim、禾莠净和tralkoxydim；咪唑啉酮类，如imazethapyr、imazamethabenz、imazapyr和imazaquin；腈类，如溴苯腈、敌草腈和碘苯腈；氧乙酰胺类，如mefenacet；磺酰脲类，如amidosulfuron、bensulfuron-methyl、chlorimuron-ethyl、阔草脲、cinosulfuron、metsulfuron-methyl、nicosulfuron、primisulfuron、pyrazosulfuron-ethyl、thifensulfuron-methyl、triasulfuron和tribenuron-metbyl 硫代氨基甲酸酯类，如苏达灭、草灭特、燕麦敌、扑草灭、esprocarb草达灭、prosulfocarb、杀草丹和野麦畏；三嗪类，如阿特拉津、草净津、西玛津、西草净、去草净和特丁津(terbutylazine)、三嗪酮类，如六嗪酮(hexazinone)、苯嗪草(metamitron)和赛克津；其他除草剂，如氨三唑、benfuresate、噻草平、cinmethylin、clomazone、clopyralid、苯敌快(difenzoquat)、dithiopyr、灭草呋喃(ethofumesate)、fluorochloridone、glufosinate、草甘膦、isoxaben、达草止(pyridate)、quinchlorac、quinmerac、sulphosate和tridiphane。
也可使用与其他已知活性化合物，如杀真菌剂、杀虫剂、杀螨剂、杀线虫剂、驱鸟剂、植物营养剂及改善土壤结构的药剂的混合物。
活性化合物可以单独使用，或以其制剂形式或通过进一步稀释由制剂形式制备的使用形式，如即用的溶液、悬浮液、乳液、粉剂、糊剂和颗粒剂使用。它们以常规方式，例如浇灌、喷雾、雾化或喷洒等方式使用。
本发明的活性化合物可以在植物出芽前或出芽后施用，也可以在播种前掺入土壤中。
活性化合物的用量可以在很大的范围内变化。这主要取决于所要求效果的性质。通常，用量为每公顷土壤表面0.001至10kg活性化合物，优选每公顷0.005至5kg活性化合物。
本发明活性化合物的制备和使用可由下列实施例示出。制备实施例实施例1
在20℃向9.7g(0.03mol)1-[N-(4-氰基-2-氟-5-异丙氧基苯基)]-四氢-(2H)-哒嗪硫代甲酰胺的150ml二氯甲烷溶液中滴加26ml(0.05mol)20％光气的甲苯溶液。将反应混合物在20℃搅拌3小时，然后将其加入约相同量的冰水中。分出有机相，用硫酸镁干燥并过滤。滤液在吸水泵抽真空状态下浓缩，残余物通过柱色谱法(硅胶，二氯甲烷)纯化。
得到1.4g(理论值的13％)9-(4-氰基-2-氟-5-异丙氧基苯基亚氨基)-8-硫杂-1，6-二氮杂双环[4.3.0]壬-7-酮，其熔点为108℃。实施例2
Figure C9411730302162
在0℃向10.8g(0.08mol)2-亚氨基哌啶盐酸盐和100ml二氯甲烷的混合物中加入3.2g(0.08mol)氢氧化钠的10ml水溶液。然后将混合物搅拌1小时，之后在0℃至5℃间滴加15.7g(0.08mol)4-氰基-2，5-二氟苯基异硫氰酸酯的150ml二氯甲烷溶液，然后将混合物在室温下搅拌3小时。然后，将反应混合物冷却到-20℃，向其中加入在40ml二氯甲烷中的12.8g(0.08mol)溴。再将该混合物搅拌3小时，之后滤掉固体，滤液依次用碳酸氢钠溶液和水洗涤。有机相经硫酸镁干燥，真空除去溶剂，剩下的固体用少量乙腈重结晶。
得到3.1g(理论量的13％)9-(4-氰基-2，5-二氟苯基亚氨基)-8-硫杂-1，7-二氨杂双环[4.3.0]壬-6-烯，其熔点为137℃。
根据本发明制备方法的一般描述，例如也可以按类似于实施例1和2的方法制备列于下表2中的式(I)化合物。表2：式(I)化合物的实施例实施例  R1  R2             A                      E             G           熔点编号                                                               (℃)3       F     NHSO2CH3     -(CH2)4-             -C＝          ＝N-4       F     O-CH(CH3)2   -(CH2)4-             -C＝          ＝N-5       F     NHSO2C2H5   -(CH2)4-             -C＝          ＝N-6       F     OCH(CH3)2    -CH2-C(CH3)2-CH2-  -C＝          ＝N-7       F     F              -CH2-CH2-CH＝CH-      N             
Figure C9411730302181
       85表2(续)实施例  R1   R2             A                      E       G             熔点编号                                                           (℃)8       F     NHSO2C3H7    -(CH2)4             -C＝     ＝N-         1409       F     F               -(CH2)4             -C＝     ＝N-          20010      F     OC2H5         -(CH2)4             -C＝     ＝N-         19411      F     OC2H5         -CH2-CH2-CH＝CH-     N       
Figure C9411730302191
     13512      F     
Figure C9411730302192
   -CH2-CH2-CH＝CH-     N       
Figure C9411730302193
 (无定形)13      F    NHSO2C2H5    -(CH2)4              N              17414      F    NHSO2CH3      -(CH2)4              N       
Figure C9411730302195
      21515      F    NHSO2C3H7    -(CH2)4              N              17616      F    OCH(CH3)2     -(CH2)4              N       
Figure C9411730302197
      106式(III)起始化合物：实施例(III-1)
Figure C9411730302201
在20℃搅拌下向2.9g(34mmol)六氢哒嗪的40ml甲苯溶液中加入8.0g(34mmol)4-氰基-2-氟-5-异丙氧基苯基异硫氰酸酯。将反应混合物在20℃搅拌16小时，然后在吸水泵抽真空状态下浓缩。
得到10.3g(理论量的94％)1-[N-(4-氰基-2-氟-5-异丙氧基苯基)]-四氢-(2H)-哒嗪硫代甲酰胺，为油状残余物，它逐渐固化成结晶形。
熔点：42℃。表3：式(III)化合物的实施例实施例       R1      R2                   A编号                                                                熔点(℃)III-2        F         F                     -CH2-CR2-CH2-CH＝  126III-3        F         OC2H4OC2H4OOH3 -CH2-CH2-CH＝CH2    58III-4        F         NHSO2CH3           -(CH2)4-III-5        F         OCH(CH3)2          -CH2-CH2-CH＝CH-     147式(VIII)起始化合物：实施例(VIII-1)
Figure C9411730302211
在约30℃和搅拌下，向由6g(0.06mol)碳酸钙、30ml水、6.9g(0.06mol)硫光气和30ml二氯甲烷组成的混合物中加入7.8g(0.04mol)4-氰基-2-氟-5-异丙氧基苯胺的25ml二氯甲烷溶液。将反应混合物在30℃至35℃之间搅拌约18小时。过滤后分离出有机相，用硫酸镁干燥并过滤。在用吸水泵抽真空状态下自滤液中小心蒸除溶剂。
得到8.4g(理论量的89％)4-氰基-2-氟-5-异丙氧基苯基异硫氰酸酯，为油状残余物，它逐渐固化成结晶形。
熔点：73℃。表4：式(VIII)化合物的实施例实施例             R1         R2           熔点编号                                         (℃)(VIII-2)           F           F             37(VIII-3)           F           NHSO2CH3    l66式(X)起始化合物：实施例X-1：
Figure C9411730302221
将由92.4g(0.6mol)4-氰基-2，5-二氟苯胺、60g(0.60mol)甲磺酰胺、166g碳酸钾和80ml N-甲基吡咯烷酮组成的混合物在180℃加热10小时。冷却后将混合物搅入5升水中，所得溶液每次用400ml乙酸乙酯洗涤两次。然后用300ml乙酸乙酯覆盖水相，并用10％盐酸酸化。将产生的结晶形产物通过吸滤而分离。
得到70g(理论量的51％)N-(5-氨基-2-氰基-4-氟苯基)甲磺酰胺，其熔点为238℃。表5：式(X)化合物的实施例实施例编号      R1            R2                    熔点
                                                   (℃)X-2             F              NH-SO2C2H5X-3             H              NHSO2CH3X-4             F              NHSO2C3H7-nX-5             F              NHSO2C3E7-isoX-6             F              
Figure C9411730302231
X-7             F               X-8             H              NH-SO2C2H5X-9             Cl             NHSO2CH3X-10            Cl             NB-SO2C2H5应用实施例实施例A芽后试验
溶剂：5份(重量)丙酮
乳化剂：1份(重量)烷基芳基聚乙二醇醚
为制备活性化合物的适当制剂，将1份(重量)活性化合物与所述量的溶剂混合，加入所述量的乳化剂，并将浓缩物用水稀释至所需浓度。
给高5-15cm的试验植物喷撒活性化合物的制剂，以此提供每单位面积所需的特定量的活性化合物。三周后，与未处理的对照样的生长相比评估对所述植物的损害程度(损害百分比)。
数字表示：
0％＝无作用(类似未处理的对照样)
100％＝完全除灭
当使用量为15g/ha时，例如在此试验中的制备实施例1的化合物表现出对杂草，如苘麻属(100％)、苋属(80％)、藜属(95％)、番薯属(100％)和婆婆纳属(85％)的强除草作用，而栽培植物对该化合物具有很好的耐受性，如大麦(0％)。实施例B芽前试验
溶剂：5份(重量)丙酮
乳化剂：1份(重量)烷基芳基聚乙二醇醚
为制备活性化合物的适当制剂，将1份(重量)活性化合物与所述量的溶剂混合，加入所述量的乳化剂，并将浓缩物用水稀释至所需浓度。
将试验植物的种子播种于常规土壤中，24小时后用上述活性化合物的制剂浇灌。合适的是将每单位面积的水量保持恒定。在制剂中上述活性化合物的浓度并不重要，只有施于每单位面积的活性化合物的量是关键性的。
三周后，与未处理的对照样的生长相比评估对所述植物的损害程度(损害百分比)。
数字表示：
0％＝无作用(类似未处理的对照样)
100％＝完全除灭
当使用量为60g/ha时，制备实施例1的化合物在此试验中表现出对下列各属的杂草很强的除草作用，如Aeopecurus(90％)、Digiteria(95％)、苘麻属(100％)、藜属(100％)、母菊属(100％)和Dinapis(80％)，而栽培植物对该化合物具有很好的耐受性，如大麦(0％)。

Claims (8)

1.通式(I)的4-氰基苯基亚氨基杂环化合物：
Figure C9411730300021
其中：
R1代表F，
R2代表-N(R4)-SO2R5，其中：
R4代表H，及
R5代表C1-C3烷基，
A代表-(CH2)4，
E代表-C＝或N，和
G代表＝N-或羰基。
2.根据权利要求1的通式(I)的4-氰基苯基亚氨基杂环化合物，其特征在于：
R1代表F，
R2代表-N(R4)-SO2R5，其中：
R4代表H，
R5代表甲基、乙基、正丙基或异丙基，
A代表-(CH2)4，
E代表-C＝或N，和
G代表＝N-或羰基。
3.根据权利要求1的通式(IA)的4-氰基苯基亚氨基杂环化合物，其特征在于：
Figure C9411730300031
其中：
R1代表F，
R2代表-N(R4)-SO2R5，其中：
R4代表H，和
R5代表C1-C3烷基，和
A代表-(CH2)4。
4.根据权利要求1的通式(IB)的4-氰基苯基亚氨基杂环化合物，其特征在于：
Figure C9411730300032
其中：
R1代表F，
R2代表-N(R4)-SO2R5，其中：
R4代表H，和
R5代表C1-C3烷基，
A代表-(CH2)4。
5.制备权利要求1的通式(I)的4-氰基苯基亚氨基杂环化合物的方法，其特征在于：
a).使通式(II)的取代的硫代羰基氨基化合物：
Figure C9411730300041
其中A、R1和R2具有权利要求1中所述定义，与氧化剂或脱氢剂任选在反应辅助剂存在下以及任选在稀释剂存在下反应，或
b).使通式(III)的取代的硫代羰基氨基化合物：
Figure C9411730300042
其中A、R1和R2具有权利要求1中所述定义，与光气任选在稀释剂存在下反应，或
c).使通式(Ia)的氰基芳基亚氨基杂环化合物：
Figure C9411730300051
其中：R1、A、E和G具有权利要求1中所述定义，和
      X1代表卤素，
与通式(V)的亲核化合物：
       H-N(R4)-SO2R5               (V)
其中：R4和R5具有权利要求1中所述定义，或与这些化合物的碱金属盐类任选在酸性接受体存在下以及任选在稀释剂存在下反应。
6.除草剂，其特征在于它含有至少一种权利要求1-2和5的式(I)的4-氰基苯基亚氨基杂环化合物。
7.权利要求1-2和5的通式(I)的4-氰基苯基亚氨基杂环化合物在防治不需要的植物方面的应用。
8.通式(II)的取代的硫代羰基氨基化合物：
Figure C9411730300052
其中：
R1代表F，
R2代表-N(R4)-SO2R5，其中：
R4代表H，
R5代表C1-C3烷基，和
A代表-(CH2)4。
CN94117303A 1993-10-18 1994-10-18 4-氰基苯基亚氨基杂环化合物 Expired - Fee Related CN1048497C (zh)

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Families Citing this family (9)

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CN1113242A (zh) * 1994-04-04 1995-12-13 住友化学工业株式会社 亚氨基噻唑啉衍生物及含有它们作为活性成分的除草剂
DE4414568A1 (de) 1994-04-27 1995-11-02 Bayer Ag Heterocyclylbenzonitrile
DE19620992A1 (de) 1996-05-24 1997-11-27 Bayer Ag Verfahren zur Herstellung von Hydroxyarenen
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TR199902243T2 (xx) * 1997-03-14 1999-12-21 Isk Americas Incorporated Diaril eterler ve bunlar� haz�rlama y�ntemleri ve bunlar� ihtiva eden herbisidal ve kurutucu madde bile�imleri.
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WO2022050621A1 (en) * 2020-09-01 2022-03-10 Samsung Electronics Co., Ltd. Intermediate structure for manufacturing micro light emitting diode display, method of manufacturing the same, and method of manufacturing micro led display

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992021684A1 (en) * 1991-06-06 1992-12-10 Ciba-Geigy Ag New herbicides
WO1993005037A1 (en) * 1991-09-04 1993-03-18 Ciba-Geigy Ag Oxetane and thiaetane derivatives

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1194835A (en) * 1966-07-07 1970-06-10 Wellcome Found Novel 1-Amidino-3-Phenyl-Urea Derivatives, the preparation thereof and Compositions containing the same
US3836506A (en) * 1970-10-30 1974-09-17 Westinghouse Electric Corp Compositions of cyanoimide polymers and heterocyclic polymers made from cyanoimide precursors
EP0238711B1 (en) * 1986-03-25 1990-11-28 Kumiai Chemical Industry Co., Ltd. Thiadiazabicyclononane derivatives, processes for their production and herbizidal compositions
DE3772364D1 (de) * 1986-12-24 1991-09-26 Kumiai Chemical Industry Co Thiadiazabicyclononanderivate und herbizide zusammensetzungen.
CA1309716C (en) * 1987-08-28 1992-11-03 Jun Satow Condensed heterocyclic derivative, process for their production and herbicides
DE3889412T2 (de) * 1987-10-16 1994-12-22 Ihara Chemical Ind Co Thiadiazabicyclononanderivate und herbizide Zubereitungen.
DE3924719A1 (de) * 1989-07-26 1991-01-31 Basf Ag Zimtsaeureester
EP0457714A1 (de) * 1990-03-22 1991-11-21 Ciba-Geigy Ag Thiadiazabicyclononanderivate, Verfahren zu ihrer Herstellung, Zwischenprodukte und ihre Verwendung als Herbizide
FR2671348B1 (fr) * 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
EP0509398B1 (de) * 1991-04-15 2001-09-19 Aventis Pharma Deutschland GmbH Chinoxaline, Verfahren zu ihrer Herstellung und ihre Verwendung
DE4131579A1 (de) * 1991-09-23 1993-03-25 Boehringer Mannheim Gmbh Thiadiazolo(4,3-a)pyridinderivate, verfahren zu ihrer herstellung und diese enthaltenden arzneimittel
EP0648749B1 (de) * 1993-08-18 1997-12-10 Bayer Ag N-Cyanoaryl-Stickstoffheterocyclen

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992021684A1 (en) * 1991-06-06 1992-12-10 Ciba-Geigy Ag New herbicides
WO1993005037A1 (en) * 1991-09-04 1993-03-18 Ciba-Geigy Ag Oxetane and thiaetane derivatives

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