WO2014041559A3 - Process for preparation of dabigatran etexilate and intermediates thereof - Google Patents

Process for preparation of dabigatran etexilate and intermediates thereof Download PDF

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Publication number
WO2014041559A3
WO2014041559A3 PCT/IN2013/000514 IN2013000514W WO2014041559A3 WO 2014041559 A3 WO2014041559 A3 WO 2014041559A3 IN 2013000514 W IN2013000514 W IN 2013000514W WO 2014041559 A3 WO2014041559 A3 WO 2014041559A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
compound
dabigatran etexilate
preparation
intermediates
Prior art date
Application number
PCT/IN2013/000514
Other languages
French (fr)
Other versions
WO2014041559A2 (en
Inventor
Sunil Kumar Singh
Shekhar Bhaskar Bhirud
Francis P D'SOUZA
Nagambar G. JAMBUKAR
Pravin THOMBRE
Amit Soni
Original Assignee
Glenmark Pharmaceuticals Limited; Glenmark Generics Limited
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 Glenmark Pharmaceuticals Limited; Glenmark Generics Limited filed Critical Glenmark Pharmaceuticals Limited; Glenmark Generics Limited
Publication of WO2014041559A2 publication Critical patent/WO2014041559A2/en
Publication of WO2014041559A3 publication Critical patent/WO2014041559A3/en

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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
    • 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

Abstract

Provided is a process for the preparation of dabigatran etexilate, a compound of Formula I or a salt thereof in a purity of at least 99.0% and wherein the level of compound of formula X and XV is less than 0.15% w/w relative to the amount of dabigatran etexilate, a compound of Formula I or a salt thereof, as determined by HPLC comprising (a) subjecting a crude compound of formula I to treatment with alkyl acetate and ketone to form a mixture; (b) optionally heating the mixture; and (c) isolating the compound of Formula I.
PCT/IN2013/000514 2012-08-27 2013-08-23 Process for the preparation of dabigatran etexilate and intermediates thereof WO2014041559A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN2481/MUM/2012 2012-08-27
IN2481MU2012 2012-08-27
US201261711663P 2012-10-09 2012-10-09
US61/711,663 2012-10-09
IN3260MU2012 2012-11-09
IN3260/MUM/2012 2012-11-09

Publications (2)

Publication Number Publication Date
WO2014041559A2 WO2014041559A2 (en) 2014-03-20
WO2014041559A3 true WO2014041559A3 (en) 2014-05-30

Family

ID=50278799

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2013/000514 WO2014041559A2 (en) 2012-08-27 2013-08-23 Process for the preparation of dabigatran etexilate and intermediates thereof

Country Status (1)

Country Link
WO (1) WO2014041559A2 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104974137A (en) * 2014-04-04 2015-10-14 江苏天士力帝益药业有限公司 New crystal forms of dabigatran etexilate mesylate and preparation method thereof
CN103965164A (en) * 2014-05-13 2014-08-06 南京生命能科技开发有限公司 Dabigatran etexilate mesylate crystals VI and preparation method thereof
CN103951654B (en) * 2014-05-13 2016-08-24 南京生命能科技开发有限公司 Crystal V of dabigatran etexilate methanesulfonate and preparation method thereof
CN105461686A (en) * 2014-08-25 2016-04-06 江苏豪森药业股份有限公司 Preparation method of high purity Pradaxa crystal form
CN105572275B (en) * 2014-10-08 2017-09-29 华仁药业股份有限公司 A kind of detection method of dabigatran etexilate methanesulfonate content
CN104356111B (en) * 2014-10-14 2017-12-26 蚌埠丰原医药科技发展有限公司 A kind of method for preparing dabigatran etcxilate mesylate hydrolysis impurity
CN105566296A (en) * 2015-12-16 2016-05-11 蚌埠丰原医药科技发展有限公司 Method for preparing dabigatran amidated impurities
CN105859686B (en) * 2016-05-24 2021-10-08 浙江华海药业股份有限公司 Refining method of dabigatran etexilate free alkali
CN106349221A (en) * 2016-08-29 2017-01-25 常州市阳光药业有限公司 Preparation method of high-purity dabigatran etexilate
CN106916141A (en) * 2017-04-06 2017-07-04 南京生命能科技开发有限公司 A kind of preparation method of dabigatran etexilate methanesulfonate
CN109975448B (en) * 2017-12-28 2022-05-20 成都倍特药业股份有限公司 Method for detecting related substances or/and content of dabigatran etexilate mesylate or preparation thereof
CN110878083A (en) * 2018-09-05 2020-03-13 连云港恒运药业有限公司 Purification method of dabigatran etexilate intermediate
CN117043150A (en) * 2021-03-22 2023-11-10 天津睿创康泰生物技术有限公司 New crystal form of dabigatran etexilate ethyl ester hydrochloride as well as preparation method and application thereof
CN113307792A (en) * 2021-05-21 2021-08-27 杭州国瑞生物科技有限公司 Refining method of dabigatran etexilate and control method of specific degradation impurities of dabigatran etexilate
CN115508479B (en) * 2022-06-24 2023-07-07 常州制药厂有限公司 Derivatization analysis method of n-hexyl chloroformate

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037075A1 (en) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, their production and use as medicaments
WO2010045900A1 (en) * 2008-10-24 2010-04-29 Zentiva, K.S. A method for the preparation of dabigatran and its intermediates
CN102050814A (en) * 2009-11-06 2011-05-11 北京美倍他药物研究有限公司 Ester derivatives of dabigatran
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037075A1 (en) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, their production and use as medicaments
WO2010045900A1 (en) * 2008-10-24 2010-04-29 Zentiva, K.S. A method for the preparation of dabigatran and its intermediates
CN102050814A (en) * 2009-11-06 2011-05-11 北京美倍他药物研究有限公司 Ester derivatives of dabigatran
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts

Also Published As

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