UA102248C2 - Способ получения дабигатрана - Google Patents

Способ получения дабигатрана

Info

Publication number
UA102248C2
UA102248C2 UAA201012170A UAA201012170A UA102248C2 UA 102248 C2 UA102248 C2 UA 102248C2 UA A201012170 A UAA201012170 A UA A201012170A UA A201012170 A UAA201012170 A UA A201012170A UA 102248 C2 UA102248 C2 UA 102248C2
Authority
UA
Ukraine
Prior art keywords
reaction
dabigatran
formula
converted
subjected
Prior art date
Application number
UAA201012170A
Other languages
English (en)
Ukrainian (uk)
Inventor
Йосеф Ирман
Индржих Рихтер
Петр Лустиг
Original Assignee
Зентива, К.С.
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
Application filed by Зентива, К.С. filed Critical Зентива, К.С.
Publication of UA102248C2 publication Critical patent/UA102248C2/ru

Links

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Способ получения дабигатрана формулы VIII, в котором продукт реакции хлорида 4-этиламино-3-нитробензоилхлорида с этил-3-(пиридин-2-иламино)пропаноатом превращают в гидрохлорид, используя раствор хлорида водорода для образования соединения формулы III-HCl, в котором нитрогруппу восстанавливают путем реакции с дитионитом натрия, и полученное соединение формулы IV подвергают взаимодействию с [( 4-цианофенил)амино]уксусной кислотой и щавелевой кислотой, продукт этого взаимодействия VI-оксал подвергают гидролизу и взаимодействию с карбонатом аммония для образования промежуточного соединения формулы VII-HCl, которое далее превращают в дабигатран реакцией с гексилхлорформиатом.
UAA201012170A 2008-03-14 2009-03-10 Способ получения дабигатрана UA102248C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CZ2008-165A CZ305085B6 (cs) 2008-03-14 2008-03-14 Způsob přípravy dabigatranu
PCT/CZ2009/000037 WO2009111997A1 (en) 2008-03-14 2009-03-10 A method for the preparation of dabigatran

Publications (1)

Publication Number Publication Date
UA102248C2 true UA102248C2 (ru) 2013-06-25

Family

ID=40627441

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201012170A UA102248C2 (ru) 2008-03-14 2009-03-10 Способ получения дабигатрана

Country Status (6)

Country Link
US (1) US8394961B2 (ru)
EP (1) EP2262771A1 (ru)
CZ (1) CZ305085B6 (ru)
EA (1) EA018053B1 (ru)
UA (1) UA102248C2 (ru)
WO (1) WO2009111997A1 (ru)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2008669A3 (cs) * 2008-10-24 2010-05-05 Zentiva, A. S. Zpusob prípravy dabigatranu a jeho meziprodukty
WO2012004397A1 (en) 2010-07-09 2012-01-12 Esteve Química, S.A. Intermediates and process for preparing a thrombin specific inhibitor
EP2937343A1 (en) 2010-07-09 2015-10-28 Esteve Química, S.A. Process of preparing a thrombin specific inhibitor
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts
HUP1100244A2 (hu) * 2011-05-11 2012-11-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag Gyógyszeripari intermedierek és eljárás elõállításukra
WO2013024384A1 (en) * 2011-08-12 2013-02-21 Alembic Pharmaceuticals Limited Improved process for preparation of dabigatran etexilate and its novel intermediate
EP2834224B1 (en) 2012-04-02 2018-06-06 MSN Laboratories 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
WO2014048958A1 (en) 2012-09-27 2014-04-03 Bayer Cropscience Ag Process for the preparation of optionally substituted phenyl and pyridyl pyrrolidines
WO2014068587A2 (en) * 2012-10-29 2014-05-08 Biophore India Pharmaceuticals Pvt. Ltd. An improved process for the synthesis of dabigatran and its intermediates
US10077251B2 (en) 2012-10-29 2018-09-18 Biophore India Pharmaceuticals Pvt. Ltd. Process for the synthesis of Dabigatran Etexilate and its intermediates
WO2015124764A1 (en) * 2014-02-24 2015-08-27 Erregierre S.P.A. Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate
WO2015128875A2 (en) * 2014-02-26 2015-09-03 Megafine Pharma (P) Ltd. A process for preparation of dabigatran etexilate mesylate and intermediates thereof
WO2015132794A1 (en) * 2014-03-06 2015-09-11 Symed Labs Limited Improved processes for the preparation of dabigatran etexilate using novel intermediates
CN103992241B (zh) * 2014-06-05 2016-08-24 雅本化学股份有限公司 N-取代苯基甘氨酸的制备方法
WO2016000230A1 (zh) 2014-07-03 2016-01-07 上海医药工业研究院 一种达比加群酯中间体的制备方法及中间体化合物
CN105461688B (zh) * 2014-08-26 2017-12-29 上海医药工业研究院 苯并咪唑化合物k的合成方法
CN108727334B (zh) * 2018-07-12 2020-10-30 江西国药有限责任公司 一种甲磺酸达比加群酯的生产工艺
CN109942434A (zh) * 2019-03-26 2019-06-28 山东世纪阳光科技有限公司 一种大红色基g的生产方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
EP1609784A1 (de) * 2004-06-25 2005-12-28 Boehringer Ingelheim Pharma GmbH & Co.KG Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen
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
EP1956018A1 (de) * 2007-02-06 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung eines Benzimidazolderivats

Also Published As

Publication number Publication date
EP2262771A1 (en) 2010-12-22
US8394961B2 (en) 2013-03-12
EA018053B1 (ru) 2013-05-30
EA201001394A1 (ru) 2011-02-28
WO2009111997A1 (en) 2009-09-17
CZ305085B6 (cs) 2015-04-29
US20110082299A1 (en) 2011-04-07
CZ2008165A3 (cs) 2009-09-23

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