CO4780028A1 - Procedimiento para la preparacion de sildenafil - Google Patents

Procedimiento para la preparacion de sildenafil

Info

Publication number
CO4780028A1
CO4780028A1 CO97032741A CO97032741A CO4780028A1 CO 4780028 A1 CO4780028 A1 CO 4780028A1 CO 97032741 A CO97032741 A CO 97032741A CO 97032741 A CO97032741 A CO 97032741A CO 4780028 A1 CO4780028 A1 CO 4780028A1
Authority
CO
Colombia
Prior art keywords
preparation
sildenafil
procedure
cyclization
compound
Prior art date
Application number
CO97032741A
Other languages
English (en)
Inventor
Peter James Dunn
Albert Shaw Wood
Original Assignee
Pfizer Res & Dev
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10795332&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO4780028(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Res & Dev filed Critical Pfizer Res & Dev
Publication of CO4780028A1 publication Critical patent/CO4780028A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)

Abstract

Un procedimiento para la preparación de un compuesto de fórmula (I):que comprende la ciclación de un compuesto de fórmula (II):donde la ciclación se realiza en condiciones básicas, neutras o ácidas.
CO97032741A 1996-06-14 1997-06-13 Procedimiento para la preparacion de sildenafil CO4780028A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9612514.1A GB9612514D0 (en) 1996-06-14 1996-06-14 Novel process

Publications (1)

Publication Number Publication Date
CO4780028A1 true CO4780028A1 (es) 1999-05-26

Family

ID=10795332

Family Applications (1)

Application Number Title Priority Date Filing Date
CO97032741A CO4780028A1 (es) 1996-06-14 1997-06-13 Procedimiento para la preparacion de sildenafil

Country Status (48)

Country Link
US (2) US5955611A (es)
EP (2) EP0812845B1 (es)
JP (2) JP2866841B2 (es)
KR (1) KR100207352B1 (es)
CN (2) CN1106399C (es)
AP (1) AP717A (es)
AR (1) AR003401A1 (es)
AT (2) ATE246194T1 (es)
AU (1) AU697684B2 (es)
BG (1) BG62554B1 (es)
BR (1) BR9703580A (es)
CA (1) CA2207694C (es)
CO (1) CO4780028A1 (es)
CZ (1) CZ290942B6 (es)
DE (2) DE69723846T2 (es)
DK (2) DK0812845T3 (es)
DZ (1) DZ2247A1 (es)
EA (1) EA000102B1 (es)
EG (1) EG24123A (es)
ES (2) ES2201397T3 (es)
GB (1) GB9612514D0 (es)
GR (1) GR3031087T3 (es)
HK (1) HK1033459A1 (es)
HN (1) HN1997000072A (es)
HR (1) HRP970326B1 (es)
HU (1) HU224497B1 (es)
ID (1) ID18745A (es)
IL (3) IL125411A (es)
IN (5) IN187350B (es)
IS (2) IS1922B (es)
MA (1) MA24205A1 (es)
MX (1) MX9704433A (es)
NO (2) NO304551B1 (es)
NZ (1) NZ328084A (es)
OA (1) OA10426A (es)
PE (2) PE1299A1 (es)
PL (1) PL189333B1 (es)
PT (1) PT916675E (es)
RS (2) RS49653B (es)
SA (1) SA97180124B1 (es)
SG (1) SG50024A1 (es)
SI (2) SI0812845T1 (es)
SK (5) SK283895B6 (es)
TN (1) TNSN97102A1 (es)
TR (1) TR199700470A2 (es)
UA (1) UA27085C2 (es)
UY (2) UY24585A1 (es)
ZA (1) ZA975259B (es)

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CN1281588C (zh) 1997-04-25 2006-10-25 美国辉瑞有限公司 制备吡唑并嘧啶酮类化合物的新型中间体
EP0992240A4 (en) * 1997-05-29 2003-04-16 Mochida Pharm Co Ltd THERAPEUTIC AGENT FOR TREATING ANERECTION
US6399618B1 (en) 1997-07-09 2002-06-04 Cardiome Pharma Corp Compositions and methods for modulating sexual activity
GB9722520D0 (en) 1997-10-24 1997-12-24 Pfizer Ltd Compounds
CN100430396C (zh) 1997-11-12 2008-11-05 拜耳医药保健股份公司 用作磷酸二酯酶抑制剂的2-苯基取代的咪唑并三嗪酮
US6251904B1 (en) * 1998-04-20 2001-06-26 Pfizer Inc. Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
CA2235642C (en) 1998-05-15 2007-11-13 Torcan Chemical Ltd. Processes for preparing sildenafil
ES2220109T3 (es) * 1998-09-04 2004-12-01 Ortho-Mcneil Pharmaceutical, Inc. 5-heterociclilpirazolo (4,3-d) pirimidin-7-onas para el tratamiento de la disfuncion erectil masculina.
GB9822238D0 (en) * 1998-10-12 1998-12-09 Pfizer Ltd Process for preparation of pyrazolo[4,3-D]pyrimidin-7-ones and intermediates thereof
GB9823103D0 (en) * 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
GB9823102D0 (en) 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
GB9823101D0 (en) 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
KR100353014B1 (ko) * 1998-11-11 2002-09-18 동아제약 주식회사 발기부전 치료에 효과를 갖는 피라졸로피리미디논 화합물
US6087362A (en) * 1999-03-16 2000-07-11 Pentech Pharmaceuticals, Inc. Apomorphine and sildenafil composition
WO2000078760A1 (fr) * 1999-06-21 2000-12-28 The Biochemical Pharmaceutical Factory Of Zhuhai Sez Procede de preparation de sildenafil, agent et procede d'obtention d'un comprime mixte a base de sildenafil et de chlorhydrate d'apomorphine
CN1094492C (zh) * 1999-06-21 2002-11-20 杭州神鹰医药化工有限公司 西地那非的制备方法
CN1077108C (zh) * 1999-07-13 2002-01-02 成都地奥制药集团有限公司 用于制备药物昔多芬的前体化合物
WO2001019827A1 (en) * 1999-09-13 2001-03-22 Cipla Ltd. A novel process for the synthesis of sildenafil citrate
US6075028A (en) * 1999-09-23 2000-06-13 Graham; Richard Method of treating Tourette's syndrome and related CNS disorders
EA200200240A1 (ru) 1999-10-11 2002-10-31 Пфайзер Инк. 5-(2-ЗАМЕЩЕННЫЕ-5-ГЕТЕРОЦИКЛИЛСУЛЬФОНИЛПИРИД-3-ИЛ)-ДИГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-7-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОДИЭСТЕРАЗЫ
TWI265925B (en) 1999-10-11 2006-11-11 Pfizer Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
YU84702A (sh) * 2000-06-22 2005-09-19 Pfizer Inc. Novi postupak za pripremanje pirazolopirimidinona
US6667398B2 (en) 2000-06-22 2003-12-23 Pfizer Inc Process for the preparation of pyrazolopyrimidinones
US6730786B2 (en) * 2000-06-22 2004-05-04 Pfizer Inc Process for the preparation of pyrazolopyrimidinones
GB0015462D0 (en) * 2000-06-22 2000-08-16 Pfizer Ltd Novel process for the preparation of pyrazolopyrimidinones
YU51701A (sh) * 2000-07-28 2003-12-31 Pfizer Inc. Postupak za dobijanje jedinjenja pirazola/4,3-d/ pirimidin-7-ona i njihovih derivata
EP1176142A1 (en) * 2000-07-28 2002-01-30 Pfizer Inc. Process for the preparation of pyrazoles
US6407259B1 (en) 2000-07-28 2002-06-18 Pfizer Inc. Process for the preparation of pyrazoles
US6821978B2 (en) 2000-09-19 2004-11-23 Schering Corporation Xanthine phosphodiesterase V inhibitors
CN1127506C (zh) * 2001-06-29 2003-11-12 刘宝顺 一种治疗阳痿的新化合物
CA2457944C (en) * 2001-08-28 2009-09-29 Schering Corporation Polycyclic guanine phosphodiesterase v inhibitors
EP1719772A1 (en) 2002-05-31 2006-11-08 Schering Corporation Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof
DE10232113A1 (de) 2002-07-16 2004-01-29 Bayer Ag Vardenafil Hydrochlorid Trihydrat enthaltende Arzneimittel
CN100374441C (zh) 2003-06-06 2008-03-12 天津倍方科技发展有限公司 二氢吡咯[2，3-d]嘧啶-4-酮衍生物，其制备方法及其制药用途
CN100360531C (zh) * 2003-12-18 2008-01-09 中国人民解放军军事医学科学院放射与辐射医学研究所 用于预防或治疗阳萎和性冷淡的新吡唑并嘧啶类化合物
EP1779852A3 (en) * 2004-01-05 2007-05-09 Teva Pharmaceutical Industries Ltd. Processes for the production of sildenafil base and citrate salt
WO2005067936A2 (en) * 2004-01-05 2005-07-28 Teva Pharmaceutical Industries Ltd. Methods for the production of sildenafil base and citrate salt
DE102005009240A1 (de) 2005-03-01 2006-09-07 Bayer Healthcare Ag Arzneiformen mit verbesserten pharmakokinetischen Eigenschaften
WO2008074194A1 (fr) * 2006-12-21 2008-06-26 Topharman Shanghai Co., Ltd. Procédé de préparation du sildénafil et de ses intermédiaires
ES2310144B1 (es) 2007-06-15 2010-01-12 Galenicum Health, S.L. Intermedios para la preparacion de un inhibidor de la fosfodiesterasa tipo 5.
BRPI0823356A2 (pt) 2008-12-12 2015-06-16 Rhein Siegfried Sa De Cv Composição de liberação pulsátil de sildenafil e processo para prepará-la
MX2010006227A (es) 2010-06-07 2011-12-14 World Trade Imp Exp Wtie Ag Nuevos derivados 1,4-diazepanos, inhibidores de pde-5.
CN102993205B (zh) * 2012-12-27 2015-04-15 华润赛科药业有限责任公司 一种高收率制备高纯度西地那非游离碱的纯化方法
CN103044330B (zh) * 2013-01-14 2018-11-13 常州亚邦制药有限公司 西地那非中间体4-氨基-1-甲基-3-正丙基吡唑-5-甲酰胺的绿色合成新工艺
CN105085526B (zh) * 2014-05-15 2017-08-01 重庆圣华曦药业股份有限公司 一种改进的西地那非制备方法
CN105753870B (zh) * 2016-04-01 2018-05-22 重庆康刻尔制药有限公司 一种西地那非杂质f及其制备方法和应用
WO2017168174A1 (en) 2016-04-02 2017-10-05 N4 Pharma Uk Limited New pharmaceutical forms of sildenafil
CN105837578A (zh) * 2016-04-05 2016-08-10 重庆康刻尔制药有限公司 一种西地那非杂质d的合成方法
WO2018069316A2 (en) 2016-10-10 2018-04-19 Transgene Sa Immunotherapeutic product and mdsc modulator combination therapy
CN113493459B (zh) * 2020-04-07 2022-12-13 广州白云山医药集团股份有限公司白云山制药总厂 Pde5抑制剂化合物及其制备方法和应用
CN112961160A (zh) * 2021-03-05 2021-06-15 遂成药业股份有限公司 一种西地那非的改良合成工艺
CN113754612B (zh) * 2021-10-26 2023-09-26 山东安舜制药有限公司 一种西地那非中间体的制备方法

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Also Published As

Publication number Publication date
GB9612514D0 (en) 1996-08-14
TNSN97102A1 (fr) 2005-03-15
IN187319B (es) 2002-03-23
PT916675E (pt) 2003-11-28
ES2201397T3 (es) 2004-03-16
SK283895B6 (sk) 2004-04-06
TR199700470A2 (xx) 1998-01-21
IL121000A0 (en) 1997-11-20
IS1923B (is) 2004-03-15
IN187320B (es) 2002-03-23
HN1997000072A (es) 1997-12-26
ZA975259B (en) 1997-12-15
HRP970326A2 (en) 1998-06-30
IL121000A (en) 2000-02-29
SI0916675T1 (en) 2003-12-31
US5955611A (en) 1999-09-21
NZ328084A (en) 1998-08-26
IN187350B (es) 2002-03-30
SK283893B6 (sk) 2004-04-06
HU9701048D0 (en) 1997-08-28
IN187317B (es) 2002-03-23
EP0812845B1 (en) 1999-07-14
AP717A (en) 1999-01-04
BR9703580A (pt) 1998-11-10
CZ290942B6 (cs) 2002-11-13
US6066735A (en) 2000-05-23
HRP970326B1 (en) 2000-10-31
KR100207352B1 (en) 1999-07-15
PL189333B1 (pl) 2005-07-29
IL125411A0 (en) 1999-03-12
IL125411A (en) 2000-02-29
UY24612A1 (es) 2000-09-29
EA199700061A1 (ru) 1997-12-30
UY24585A1 (es) 1997-12-02
ATE182150T1 (de) 1999-07-15
ATE246194T1 (de) 2003-08-15
NO972481L (no) 1997-12-15
SI0812845T1 (en) 1999-12-31
EA000102B1 (ru) 1998-08-27
PE1299A1 (es) 1999-01-13
IS4503A (is) 1997-12-15
CA2207694C (en) 1999-11-23
HU224497B1 (hu) 2005-10-28
CA2207694A1 (en) 1997-12-14
IS6634A (is) 2002-11-25
SA97180124A (ar) 2005-12-03
AU2487897A (en) 1997-12-18
DZ2247A1 (fr) 2002-12-18
NO306115B1 (no) 1999-09-20
NO304551B1 (no) 1999-01-11
JP3058863B2 (ja) 2000-07-04
PL320555A1 (en) 1997-12-22
HUP9701048A2 (hu) 1998-12-28
BG101569A (en) 1998-01-30
AU697684B2 (en) 1998-10-15
SA97180124B1 (ar) 2006-02-08
MX9704433A (es) 1998-11-30
CZ181197A3 (cs) 1998-03-18
SG50024A1 (en) 1998-06-15
EP0812845A1 (en) 1997-12-17
CN1282740A (zh) 2001-02-07
DE69723846T2 (de) 2004-03-04
DE69723846D1 (de) 2003-09-04
EP0916675A3 (en) 1999-07-14
SK283894B6 (sk) 2004-04-06
YU25497A (sh) 1998-12-23
SK283897B6 (sk) 2004-04-06
HK1033459A1 (en) 2001-08-31
NO972481D0 (no) 1997-05-30
RS20060484A (en) 2007-04-10
CN1149206C (zh) 2004-05-12
RS49924B (sr) 2008-09-29
DE69700321D1 (de) 1999-08-19
UA27085C2 (uk) 2000-02-28
IN187318B (es) 2002-03-23
JP2866841B2 (ja) 1999-03-08
IS1922B (is) 2004-03-15
SK74397A3 (en) 1998-06-03
JPH1081688A (ja) 1998-03-31
EP0916675A2 (en) 1999-05-19
GR3031087T3 (en) 1999-12-31
NO985064L (no) 1997-12-15
SK283896B6 (sk) 2004-04-06
CN1168376A (zh) 1997-12-24
NO985064D0 (no) 1998-10-30
AP9701009A0 (en) 1997-07-31
ID18745A (id) 1998-05-07
DE69700321T2 (de) 1999-11-04
BG62554B1 (bg) 2000-02-29
EG24123A (en) 2008-07-06
ES2134051T3 (es) 1999-09-16
OA10426A (en) 2001-12-07
JPH11171879A (ja) 1999-06-29
EP0916675B1 (en) 2003-07-30
KR980002051A (ko) 1998-03-30
DK0916675T3 (da) 2003-10-27
MA24205A1 (fr) 1997-12-31
AR003401A1 (es) 1998-08-05
HUP9701048A3 (en) 2000-10-30
RS49653B (sr) 2007-09-21
CN1106399C (zh) 2003-04-23
DK0812845T3 (da) 1999-11-29
PE20011303A1 (es) 2001-12-25

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