BR9813022A - Derivados de ésteres hidroxiacéticos, seu processo de preparação e sua utilização como intermediários de sìntese - Google Patents
Derivados de ésteres hidroxiacéticos, seu processo de preparação e sua utilização como intermediários de sìnteseInfo
- Publication number
- BR9813022A BR9813022A BR9813022-6A BR9813022A BR9813022A BR 9813022 A BR9813022 A BR 9813022A BR 9813022 A BR9813022 A BR 9813022A BR 9813022 A BR9813022 A BR 9813022A
- Authority
- BR
- Brazil
- Prior art keywords
- derivatives
- preparation process
- esters
- synthesis intermediates
- synthesis
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 150000002148 esters Chemical class 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 3
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 abstract 1
- 229960003009 clopidogrel Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
- C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
- C07C309/66—Methanesulfonates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
- Cephalosporin Compounds (AREA)
Abstract
Patente de Invenção:<B>"DERIVADOS DE éSTERES HIDROXIACéTICOS, SEU PROCESSO DE PREPARAçãO E SUA UTILIZAçãO COMO INTERMEDIáRIOS DE SìNTESE"<D>. A invenção refere-se aos derivados de ésteres (R)-sulfoniloxiacéticos de fórmula geral (I); na qual R~ 1~ representa um grupamento benzila, alquila com C~ 1~-C~ 4~ eventualmente substituído por um ou vários átomos de halogênio, ou fenila eventualmente substituído por um ou vários átomos de halogênio ou por um ou vários grupamentos alquilas, lineares ou ramificados, com C~ 1~-C~ 4~ ou por um grupamento nitro. Esses compostos são intermediários na síntese do clopidogrel.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9712441A FR2769313B1 (fr) | 1997-10-06 | 1997-10-06 | Derives d'esters hydroxyacetiques, leur procede de preparation et leur utilisation comme intermediaires de synthese |
PCT/FR1998/002082 WO1999018110A1 (fr) | 1997-10-06 | 1998-09-29 | Derives d'esters hydroxyacetiques, leur procede de preparation et leur utilisation comme intermediaires de synthese |
Publications (2)
Publication Number | Publication Date |
---|---|
BR9813022A true BR9813022A (pt) | 2000-08-15 |
BR9813022B1 BR9813022B1 (pt) | 2010-07-13 |
Family
ID=9511879
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI9813022-6A BR9813022B1 (pt) | 1997-10-06 | 1998-09-29 | derivados de ésteres hidroxiacéticos, seu processo de preparação e sua utilização como intermediários de sìntese. |
Country Status (15)
Country | Link |
---|---|
US (3) | US6573381B1 (pt) |
EP (1) | EP1021449B1 (pt) |
JP (3) | JP3827946B2 (pt) |
AT (1) | ATE211476T1 (pt) |
AU (1) | AU9354498A (pt) |
BR (1) | BR9813022B1 (pt) |
CA (1) | CA2306409C (pt) |
DE (1) | DE69803397T2 (pt) |
DK (1) | DK1021449T3 (pt) |
ES (1) | ES2171040T3 (pt) |
FR (1) | FR2769313B1 (pt) |
HU (1) | HU226771B1 (pt) |
NO (1) | NO325150B1 (pt) |
PT (1) | PT1021449E (pt) |
WO (1) | WO1999018110A1 (pt) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002018357A1 (en) * | 2000-08-29 | 2002-03-07 | Rpg Life Sciences Limited | A ONE-POT PROCESS FOR THE PREPARATION OF PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS OF 4, 5, 6, 7 - TETRAHYDROTHIENO (3,2-c) PYRIDINE DERIVATIVES HAVING ANTITHROMBOTIC ACTIVITY |
US6495691B1 (en) | 2001-07-06 | 2002-12-17 | Brantford Chemicals Inc. | Process for the preparation of tetrahydrothieno[3,2-c]pyridine derivatives |
US6767913B2 (en) | 2001-12-18 | 2004-07-27 | Teva Pharmaceutical Industries Ltd. | Crystal forms iii, iv, v, and novel amorphous form of clopidogrel hydrogensulfate, processes for their preparation, processes for the preparation of form i, compositions containing the new forms and methods of administering the new forms |
MXPA04006088A (es) * | 2001-12-18 | 2004-09-27 | Teva Pharma | Polimorfo de sulfato de hidrogeno de clopidogrel. |
US7074928B2 (en) | 2002-01-11 | 2006-07-11 | Teva Pharmaceutical Industries, Ltd. | Polymorphs of clopidogrel hydrogensulfate |
ITMI20020933A1 (it) * | 2002-05-03 | 2003-11-03 | Danimite Dipharma S P A | Procedimento per la sintesi di clopidogrel |
IL166593A0 (en) | 2002-08-02 | 2006-01-15 | Racemization and enantiomer separation of clopidogrel | |
US6800759B2 (en) | 2002-08-02 | 2004-10-05 | Teva Pharmaceutical Industries Ltd. | Racemization and enantiomer separation of clopidogrel |
ITMI20022228A1 (it) * | 2002-10-21 | 2004-04-22 | Dinamite Dipharma S P A | Sali di clopidogrel con acidi alchil-solforici. |
EP1603920A1 (en) | 2003-03-12 | 2005-12-14 | Cadila Healthcare Ltd. | Polymorph and amorphous form of (s)-(+)-clopidogrel bisulfate |
WO2004098593A1 (en) * | 2003-05-05 | 2004-11-18 | Hetero Drugs Limited | Amorphous clopidogrel hydrogen sulfate composition |
US8907090B2 (en) | 2003-11-03 | 2014-12-09 | Cadila Healthcare Limited | Processes for preparing different forms of (S)-(+)-Clopidogrel bisulfate |
EP1589019B1 (de) | 2004-04-20 | 2008-08-13 | Ratiopharm GmbH | Stereoselektives Verfahren zur Herstellung von Clopidogrel |
CZ20041048A3 (cs) * | 2004-10-18 | 2005-11-16 | Zentiva, A. S | Způsob výroby klopidogrelu |
CN100406568C (zh) * | 2005-02-18 | 2008-07-30 | 淮北市辉克药业有限公司 | 氯吡格雷新生产工艺 |
WO2007032023A2 (en) * | 2005-07-12 | 2007-03-22 | Rpg Life Sciences Limited | A process for preparation of methyl-(+)-(s)-alpha-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4h)-acetic acid methyl ester or salts thereof having higher chiral purity and products thereof |
US20080311636A1 (en) * | 2005-09-02 | 2008-12-18 | Daiichi Fine Chemical Co., Ltd. | Method for Producing Optically Active Alpha-Hydroxycarboxylic Acid |
KR101235117B1 (ko) | 2005-12-26 | 2013-02-20 | 에스케이케미칼주식회사 | 광학분리에 의한 (s)-(+)-클로피도그렐의 제조방법 |
WO2007144729A1 (en) * | 2006-06-13 | 2007-12-21 | Orchid Chemicals & Pharmaceuticals Limited | An improved process for the preparation of clopidogrel |
WO2008004249A2 (en) * | 2006-07-04 | 2008-01-10 | Msn Laboratories Limited | An improved process for the preparation of clopidogrel and its pharmaceutically acceptable salts |
ATE488520T1 (de) * | 2006-08-04 | 2010-12-15 | Merz Pharma Gmbh & Co Kgaa | Pyrazolopyrimidine, ein verfahren zu ihrer herstellung und ihre verwendung als medizin |
KR100834967B1 (ko) * | 2006-08-11 | 2008-06-03 | 에스케이케미칼주식회사 | 여액의 라세미화 반응에 의한 s-(+)-클로피도그렐의고수율 제조방법 |
EP1980563A1 (en) | 2007-04-09 | 2008-10-15 | BATTULA, Srinivasa Reddy | Procedure for the preparation of methyl (+)-(S)-Alpha-(O-chlorophenyl)-6,7-dihydrothieno-[3,2-C]pyridine-5(4H) acetate |
KR20090086903A (ko) * | 2007-04-18 | 2009-08-14 | 테바 파마슈티컬 인더스트리즈 리미티드 | 개선된 클로피도그렐의 제조 방법 |
KR20150041173A (ko) | 2007-04-27 | 2015-04-15 | 사이덱스 파마슈티칼스, 인크. | 클로피도그렐 및 설포알킬 에테르 사이클로덱스트린을 함유하는 제형 및 사용 방법 |
EP2107061A1 (en) | 2008-04-02 | 2009-10-07 | Krka Tovarna Zdravil, D.D., Novo Mesto | Process for the preparation of optically enriched clopidogrel |
KR100990949B1 (ko) | 2008-06-09 | 2010-10-29 | 엔자이텍 주식회사 | 클로피도그렐 및 그의 유도체의 제조방법 |
KR101743591B1 (ko) | 2009-05-13 | 2017-06-20 | 사이덱스 파마슈티칼스, 인크. | 프라수그렐 및 사이클로덱스트린 유도체를 포함하는 약학 조성물 및 그의 제조 및 사용 방법 |
CN102120744B (zh) * | 2010-02-02 | 2013-01-09 | 江苏威凯尔医药科技有限公司 | 光学活性2-羟基四氢噻吩并吡啶衍生物及其制备方法与在制药中的用途 |
CN102558138A (zh) * | 2010-12-08 | 2012-07-11 | 湖北成田制药股份有限公司 | 2-卤代苯基-2-(2-噻吩乙氨基)乙酸酯类及其盐的制备方法 |
WO2012123958A1 (en) | 2011-02-14 | 2012-09-20 | Cadila Healthcare Limited | Highly pure salts of clopidogrel free of genotoxic impurities |
CN102351877B (zh) * | 2011-08-12 | 2014-07-09 | 天津药物研究院 | 噻吩衍生物、其制备方法和用途 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2530247B1 (fr) * | 1982-07-13 | 1986-05-16 | Sanofi Sa | Nouveaux derives de la thieno (3, 2-c) pyridine, leur procede de preparation et leur application therapeutique |
FR2623810B2 (fr) * | 1987-02-17 | 1992-01-24 | Sanofi Sa | Sels de l'alpha-(tetrahydro-4,5,6,7 thieno(3,2-c) pyridyl-5) (chloro-2 phenyl) -acetate de methyle dextrogyre et compositions pharmaceutiques en contenant |
US5189170A (en) | 1989-09-29 | 1993-02-23 | Sanofi | Process for the preparation of phenylacetic derivatives of thieno-pyridines |
FR2652575B1 (fr) * | 1989-09-29 | 1992-01-24 | Sanofi Sa | Procede de preparation d'acides alpha-bromo phenylacetiques. |
FR2664276B1 (fr) * | 1990-07-04 | 1992-10-23 | Sanofi Sa | Derive thienyl-2 glycidique, son procede de preparation et son utilisation comme intermediaire de synthese. |
FR2664596B1 (fr) * | 1990-07-10 | 1994-06-10 | Sanofi Sa | Procede de preparation d'un derive n-phenylacetique de tetrahydrothieno [3,2-c] pyridine et son intermediaire de synthese. |
JPH06293729A (ja) * | 1993-04-06 | 1994-10-21 | Sankyo Co Ltd | 光学活性カルボン酸誘導体 |
US5583147A (en) * | 1994-03-23 | 1996-12-10 | The Dupont Merck Pharmaceutical Company | Amides for the treatment of atherosclerosis |
FR2751540B1 (fr) * | 1996-07-26 | 1998-10-16 | Sanofi Sa | Composition pharmaceutique antithrombotique |
HU222283B1 (hu) * | 1997-05-13 | 2003-05-28 | Sanofi-Synthelabo | Eljárás tieno[3,2-c]piridin-származékok előállítására |
-
1997
- 1997-10-06 FR FR9712441A patent/FR2769313B1/fr not_active Expired - Lifetime
-
1998
- 1998-09-29 WO PCT/FR1998/002082 patent/WO1999018110A1/fr active IP Right Grant
- 1998-09-29 JP JP2000514920A patent/JP3827946B2/ja not_active Expired - Lifetime
- 1998-09-29 PT PT98946523T patent/PT1021449E/pt unknown
- 1998-09-29 EP EP98946523A patent/EP1021449B1/fr not_active Expired - Lifetime
- 1998-09-29 ES ES98946523T patent/ES2171040T3/es not_active Expired - Lifetime
- 1998-09-29 DE DE69803397T patent/DE69803397T2/de not_active Expired - Lifetime
- 1998-09-29 AU AU93544/98A patent/AU9354498A/en not_active Abandoned
- 1998-09-29 CA CA2306409A patent/CA2306409C/fr not_active Expired - Lifetime
- 1998-09-29 DK DK98946523T patent/DK1021449T3/da active
- 1998-09-29 US US09/509,879 patent/US6573381B1/en not_active Expired - Lifetime
- 1998-09-29 AT AT98946523T patent/ATE211476T1/de active
- 1998-09-29 BR BRPI9813022-6A patent/BR9813022B1/pt not_active IP Right Cessation
- 1998-09-29 HU HU0004250A patent/HU226771B1/hu unknown
-
2000
- 2000-04-04 NO NO20001736A patent/NO325150B1/no not_active IP Right Cessation
-
2003
- 2003-04-29 US US10/425,437 patent/US6894186B2/en not_active Expired - Lifetime
-
2004
- 2004-07-14 US US10/890,749 patent/US7153969B2/en not_active Expired - Lifetime
-
2005
- 2005-12-20 JP JP2005366868A patent/JP4264437B2/ja not_active Expired - Lifetime
-
2009
- 2009-01-08 JP JP2009002505A patent/JP4903819B2/ja not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
HUP0004250A3 (en) | 2001-12-28 |
BR9813022B1 (pt) | 2010-07-13 |
US7153969B2 (en) | 2006-12-26 |
US6573381B1 (en) | 2003-06-03 |
JP4903819B2 (ja) | 2012-03-28 |
DK1021449T3 (da) | 2002-04-22 |
JP2009137989A (ja) | 2009-06-25 |
EP1021449A1 (fr) | 2000-07-26 |
WO1999018110A1 (fr) | 1999-04-15 |
AU9354498A (en) | 1999-04-27 |
ES2171040T3 (es) | 2002-08-16 |
JP2006124398A (ja) | 2006-05-18 |
FR2769313B1 (fr) | 2000-04-21 |
NO20001736L (no) | 2000-06-06 |
US20030208077A1 (en) | 2003-11-06 |
JP3827946B2 (ja) | 2006-09-27 |
DE69803397T2 (de) | 2002-08-29 |
PT1021449E (pt) | 2002-06-28 |
HUP0004250A2 (hu) | 2001-10-28 |
NO325150B1 (no) | 2008-02-11 |
JP4264437B2 (ja) | 2009-05-20 |
US20040260110A1 (en) | 2004-12-23 |
US6894186B2 (en) | 2005-05-17 |
HU226771B1 (en) | 2009-09-28 |
NO20001736D0 (no) | 2000-04-04 |
FR2769313A1 (fr) | 1999-04-09 |
CA2306409C (fr) | 2010-06-29 |
CA2306409A1 (fr) | 1999-04-15 |
DE69803397D1 (de) | 2002-02-28 |
EP1021449B1 (fr) | 2002-01-02 |
JP2001519353A (ja) | 2001-10-23 |
ATE211476T1 (de) | 2002-01-15 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B25D | Requested change of name of applicant approved |
Owner name: SANOFI-AVENTIS (FR) Free format text: ALTERADO DE: SANOFI-SYNTHELABO |
|
B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 13/07/2010, OBSERVADAS AS CONDICOES LEGAIS. |
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B21A | Patent or certificate of addition expired [chapter 21.1 patent gazette] |
Free format text: PATENTE EXTINTA EM 13.07.2020 |