TN2009000327A1 - Procede pour la preparation d'un derive de benzimidazole - Google Patents
Procede pour la preparation d'un derive de benzimidazoleInfo
- Publication number
- TN2009000327A1 TN2009000327A1 TNP2009000327A TN2009000327A TN2009000327A1 TN 2009000327 A1 TN2009000327 A1 TN 2009000327A1 TN P2009000327 A TNP2009000327 A TN P2009000327A TN 2009000327 A TN2009000327 A TN 2009000327A TN 2009000327 A1 TN2009000327 A1 TN 2009000327A1
- Authority
- TN
- Tunisia
- Prior art keywords
- preparation
- benzimidazole derivative
- exexilate
- synthesis
- compound
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 150000001556 benzimidazoles Chemical class 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- YBSJFWOBGCMAKL-UHFFFAOYSA-N dabigatran Chemical compound N=1C2=CC(C(=O)N(CCC(O)=O)C=3N=CC=CC=3)=CC=C2N(C)C=1CNC1=CC=C(C(N)=N)C=C1 YBSJFWOBGCMAKL-UHFFFAOYSA-N 0.000 abstract 1
- 229960003850 dabigatran Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
L'invention concerne un procédé de préparation du composé de formule 1 : un produit intermédiaire valable dans la synthèse de la substance active pharmaceutique etexilate de dabigatran.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07101822A EP1956018A1 (fr) | 2007-02-06 | 2007-02-06 | Procédé de préparation d'un dérivé du benzimidazole |
| PCT/EP2008/051397 WO2008095928A1 (fr) | 2007-02-06 | 2008-02-05 | Procédé de préparation d'un dérivé de benzimidazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TN2009000327A1 true TN2009000327A1 (fr) | 2010-12-31 |
Family
ID=38166801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TNP2009000327A TN2009000327A1 (fr) | 2007-02-06 | 2009-07-31 | Procede pour la preparation d'un derive de benzimidazole |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8119810B2 (fr) |
| EP (2) | EP1956018A1 (fr) |
| JP (1) | JP5247728B2 (fr) |
| KR (1) | KR20090116781A (fr) |
| CN (1) | CN101600709B (fr) |
| AR (1) | AR065196A1 (fr) |
| AT (1) | ATE476430T1 (fr) |
| AU (1) | AU2008212908B2 (fr) |
| BR (1) | BRPI0807197A2 (fr) |
| CA (1) | CA2675624C (fr) |
| CL (1) | CL2008000355A1 (fr) |
| CY (1) | CY1111045T1 (fr) |
| DE (1) | DE602008002057D1 (fr) |
| DK (1) | DK2118090T3 (fr) |
| EA (1) | EA015967B1 (fr) |
| EC (1) | ECSP099509A (fr) |
| ES (1) | ES2349905T3 (fr) |
| HR (1) | HRP20100458T1 (fr) |
| IL (1) | IL199330A (fr) |
| MA (1) | MA31118B1 (fr) |
| MX (1) | MX2009006834A (fr) |
| MY (1) | MY148629A (fr) |
| NZ (1) | NZ579133A (fr) |
| PE (1) | PE20081737A1 (fr) |
| PL (1) | PL2118090T3 (fr) |
| PT (1) | PT2118090E (fr) |
| SI (1) | SI2118090T1 (fr) |
| TN (1) | TN2009000327A1 (fr) |
| TW (1) | TWI417291B (fr) |
| UA (1) | UA94988C2 (fr) |
| UY (1) | UY30888A1 (fr) |
| WO (1) | WO2008095928A1 (fr) |
| ZA (1) | ZA200906050B (fr) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005061623A1 (de) * | 2005-12-21 | 2007-06-28 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verbessertes Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen und deren Salzen |
| CZ305085B6 (cs) * | 2008-03-14 | 2015-04-29 | Zentiva, K.S. | Způsob přípravy dabigatranu |
| MX2010010647A (es) * | 2008-03-28 | 2010-10-20 | Boehringer Ingelheim Int | Proceso para preparar formulaciones de dabigatran para administracion oral. |
| CA2728058C (fr) * | 2008-06-16 | 2016-05-17 | Boehringer Ingelheim International Gmbh | Procede de fabrication d'un produit intermediaire de dabigatran etexilate |
| BRPI0915942A2 (pt) | 2008-07-14 | 2019-04-09 | Boehringer Ingelheim International Gmbh | método para produção de compostos medicinais contendo dabigatrana |
| WO2010055021A1 (fr) | 2008-11-11 | 2010-05-20 | Boehringer Ingelheim International Gmbh | Procede de traitement et de prevention de la thrombose utilisant l'etexilate de dabigatran ou un sel de celui-ci avec un profil de securite ameliore par rapport a la therapie de la warfarine classique |
| CN102050814B (zh) * | 2009-11-06 | 2014-05-28 | 北京美倍他药物研究有限公司 | 达比加群的酯衍生物 |
| CN102050815B (zh) * | 2009-11-06 | 2014-04-02 | 北京美倍他药物研究有限公司 | 作为前药的达比加群的酯衍生物 |
| US8399678B2 (en) | 2009-11-18 | 2013-03-19 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dabigatran etexilate |
| US8981105B2 (en) | 2010-07-09 | 2015-03-17 | Esteve Quimica, S.A. | Process of preparing a thrombin specific inhibitor |
| US9006448B2 (en) | 2010-12-06 | 2015-04-14 | Msn Laboratories Private Limited | Process for the preparation of benzimidazole derivatives and its salts |
| CN102838588B (zh) * | 2011-06-24 | 2014-03-19 | 中国药科大学 | 一类可用于口服的凝血酶抑制剂、其制法以及医药用途 |
| CN102633713B (zh) * | 2012-03-22 | 2013-12-11 | 南京工业大学 | 达比加群酯中间体及其制备方法、以及制备达比加群酯的方法 |
| US9273030B2 (en) | 2012-04-02 | 2016-03-01 | Msn Laboratories Private Limited | Process for the preparation of benzimidazole derivatives and salts thereof |
| CN102911160B (zh) * | 2012-06-29 | 2014-10-22 | 上海奥博生物医药技术有限公司 | 一种制备和纯化达比加群酯中间体的方法 |
| JP2015522596A (ja) * | 2012-07-16 | 2015-08-06 | インテルキム、ソシエダッド アノニマ | ダビガトランエテキシラートの合成のための中間体を調製する方法及び該中間体の結晶形 |
| WO2014068587A2 (fr) * | 2012-10-29 | 2014-05-08 | Biophore India Pharmaceuticals Pvt. Ltd. | Procédé amélioré de synthèse du dabigatran et de ses intermédiaires |
| US10077251B2 (en) | 2012-10-29 | 2018-09-18 | Biophore India Pharmaceuticals Pvt. Ltd. | Process for the synthesis of Dabigatran Etexilate and its intermediates |
| CN102977077A (zh) * | 2012-11-28 | 2013-03-20 | 浙江燎原药业有限公司 | 一种达比加群酯中间体的制备方法 |
| CN103224469A (zh) * | 2013-05-16 | 2013-07-31 | 上海应用技术学院 | 一种以含氟基团修饰的苯环为中心的达比加群酯类似物及其合成方法 |
| CN103288744A (zh) * | 2013-06-04 | 2013-09-11 | 上海应用技术学院 | 一种含氟基团修饰的达比加群酯类似物及其合成方法 |
| CN104418839B (zh) * | 2013-08-26 | 2019-02-01 | 深圳翰宇药业股份有限公司 | 达比加群酯的合成方法 |
| CN103710406B (zh) * | 2013-12-05 | 2017-08-11 | 蚌埠丰原医药科技发展有限公司 | 一种酶促反应制备达比加群酯主要中间体的方法 |
| CN103772358A (zh) * | 2014-01-07 | 2014-05-07 | 万特制药(海南)有限公司 | 一种制备达比加群酯的合成方法 |
| CN104003977B (zh) * | 2014-06-05 | 2016-04-13 | 雅本化学股份有限公司 | N-(2-氯甲基-1-甲基-1h-苯并咪唑-5-酰基)-n-(吡啶-2-基) -3-氨基丙酸乙酯的制备方法 |
| CN104045628B (zh) * | 2014-06-13 | 2019-04-09 | 深圳翰宇药业股份有限公司 | 苯并咪唑衍生物的纯化方法 |
| CN105315257A (zh) * | 2014-06-24 | 2016-02-10 | 华仁药业股份有限公司 | 一种达比加群酯的合成及纯化方法 |
| WO2016000230A1 (fr) | 2014-07-03 | 2016-01-07 | 上海医药工业研究院 | Procédé de préparation d'un intermédiaire d'étexilate de dabigatran et composé intermédiaire |
| WO2016027077A1 (fr) * | 2014-08-18 | 2016-02-25 | Cipla Limited | Procédés pour la préparation d'étéxilate de dabigatran et de ses intermédiaires |
| CN104744438A (zh) * | 2014-12-17 | 2015-07-01 | 烟台东诚药业集团股份有限公司 | 一种用于合成制备达比加群酯苯并咪唑中间体的方法 |
| WO2016132296A1 (fr) * | 2015-02-18 | 2016-08-25 | Piramal Enterprises Limited | Procédé de préparation d'un produit intermédiaire d'étexilate de dabigatran |
| CN105601615A (zh) * | 2015-11-17 | 2016-05-25 | 烟台东诚药业集团股份有限公司 | 一种用于纯化公斤级达比加群酯游离碱的方法 |
| CN105330645B (zh) * | 2015-11-30 | 2020-06-02 | 常州市阳光药业有限公司 | 达比加群酯中间体的制备方法 |
| CN106866626A (zh) * | 2015-12-14 | 2017-06-20 | 天津药物研究院有限公司 | 一种达比加群酯中间体的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4632993A (en) * | 1984-10-11 | 1986-12-30 | Pfizer Inc. | Process for making 2-guanidino-4-(2-methyl-4-imidazolyl) thiazole dihydrobromide |
| JPH02283860A (ja) * | 1989-04-24 | 1990-11-21 | Nissan Motor Co Ltd | エンジンの点火時期制御装置 |
| US5233944A (en) * | 1989-08-08 | 1993-08-10 | Fuji Jukogyo Kabushiki Kaisha | Control apparatus for alcohol engine |
| GB9417310D0 (en) * | 1994-08-27 | 1994-10-19 | Pfizer Ltd | Therapeutic agents |
| PE121699A1 (es) * | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| US6414008B1 (en) * | 1997-04-29 | 2002-07-02 | Boehringer Ingelheim Pharma Kg | Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions |
| GB0014006D0 (en) * | 2000-06-08 | 2000-08-02 | Smithkline Beecham Plc | Novel pharmaceutical |
| DE10230012A1 (de) * | 2002-07-04 | 2004-01-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 5,6-Dihydro-4H-imidazo[4,5,1-ij]chinoline,ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE10235639A1 (de) * | 2002-08-02 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Prodrugs von 1-Methyl-2-(4-amidinophenylaminomethyl)-benzimidazol-5-yl-carbonsäure-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amid, ihre Herstellung und ihre Verwendung als Arzneimittel |
| EP1609784A1 (fr) * | 2004-06-25 | 2005-12-28 | Boehringer Ingelheim Pharma GmbH & Co.KG | Procédé pour la préparation de 4-(benzimidazolylméthylamino)-benzamidines |
| US7314033B2 (en) * | 2004-11-18 | 2008-01-01 | Massachusetts Institute Of Technology | Fuel management system for variable ethanol octane enhancement of gasoline engines |
| CN100509799C (zh) * | 2005-12-16 | 2009-07-08 | 复旦大学 | 一种合成非手性,非肽类的抗凝血酶抑制剂的方法 |
-
2007
- 2007-02-06 EP EP07101822A patent/EP1956018A1/fr not_active Ceased
-
2008
- 2008-02-01 UY UY30888A patent/UY30888A1/es not_active Application Discontinuation
- 2008-02-04 PE PE2008000244A patent/PE20081737A1/es not_active Application Discontinuation
- 2008-02-05 BR BRPI0807197-7A patent/BRPI0807197A2/pt not_active IP Right Cessation
- 2008-02-05 JP JP2009547712A patent/JP5247728B2/ja active Active
- 2008-02-05 DE DE602008002057T patent/DE602008002057D1/de active Active
- 2008-02-05 SI SI200830078T patent/SI2118090T1/sl unknown
- 2008-02-05 CN CN2008800039517A patent/CN101600709B/zh not_active Expired - Fee Related
- 2008-02-05 ES ES08708696T patent/ES2349905T3/es active Active
- 2008-02-05 EA EA200901039A patent/EA015967B1/ru not_active IP Right Cessation
- 2008-02-05 WO PCT/EP2008/051397 patent/WO2008095928A1/fr active Application Filing
- 2008-02-05 PT PT08708696T patent/PT2118090E/pt unknown
- 2008-02-05 TW TW097104663A patent/TWI417291B/zh not_active IP Right Cessation
- 2008-02-05 AT AT08708696T patent/ATE476430T1/de active
- 2008-02-05 US US12/525,867 patent/US8119810B2/en active Active
- 2008-02-05 KR KR1020097018468A patent/KR20090116781A/ko not_active Abandoned
- 2008-02-05 HR HR20100458T patent/HRP20100458T1/hr unknown
- 2008-02-05 NZ NZ579133A patent/NZ579133A/en not_active IP Right Cessation
- 2008-02-05 CA CA2675624A patent/CA2675624C/fr not_active Expired - Fee Related
- 2008-02-05 AU AU2008212908A patent/AU2008212908B2/en not_active Ceased
- 2008-02-05 UA UAA200908939A patent/UA94988C2/ru unknown
- 2008-02-05 DK DK08708696.3T patent/DK2118090T3/da active
- 2008-02-05 MX MX2009006834A patent/MX2009006834A/es active IP Right Grant
- 2008-02-05 MY MYPI20093227A patent/MY148629A/en unknown
- 2008-02-05 AR ARP080100495A patent/AR065196A1/es unknown
- 2008-02-05 EP EP08708696A patent/EP2118090B1/fr active Active
- 2008-02-05 CL CL200800355A patent/CL2008000355A1/es unknown
- 2008-02-05 PL PL08708696T patent/PL2118090T3/pl unknown
-
2009
- 2009-06-11 IL IL199330A patent/IL199330A/en not_active IP Right Cessation
- 2009-07-10 EC EC2009009509A patent/ECSP099509A/es unknown
- 2009-07-31 TN TNP2009000327A patent/TN2009000327A1/fr unknown
- 2009-07-31 MA MA32129A patent/MA31118B1/fr unknown
- 2009-09-01 ZA ZA200906050A patent/ZA200906050B/xx unknown
-
2010
- 2010-10-25 CY CY20101100957T patent/CY1111045T1/el unknown
-
2012
- 2012-01-17 US US13/351,621 patent/US8455650B2/en active Active
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