[go: up one dir, main page]

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

Process for preparation of dabigatran etexilate and intermediates thereof Download PDF

Info

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
Legal status (The legal status 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 status listed.)
Ceased
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glenmark Pharmaceuticals Ltd
Original Assignee
Glenmark Pharmaceuticals Ltd
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 Ltd filed Critical Glenmark Pharmaceuticals Ltd
Publication of WO2014041559A2 publication Critical patent/WO2014041559A2/en
Publication of WO2014041559A3 publication Critical patent/WO2014041559A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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 Ceased WO2014041559A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN2481MU2012 2012-08-27
IN2481/MUM/2012 2012-08-27
US201261711663P 2012-10-09 2012-10-09
US61/711,663 2012-10-09
IN3260/MUM/2012 2012-11-09
IN3260MU2012 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 Ceased 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 (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108864049A (en) * 2014-04-04 2018-11-23 江苏天士力帝益药业有限公司 Dabigatran etcxilate mesylate novel crystal forms 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
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
EP3177605B1 (en) * 2014-08-07 2019-03-27 Boehringer Ingelheim International GmbH Method for producing dabigatran etexilate methanesulphonate
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

Publication number Publication date
WO2014041559A2 (en) 2014-03-20

Similar Documents

Publication Publication Date Title
WO2014041559A3 (en) Process for preparation of dabigatran etexilate and intermediates thereof
WO2013040286A3 (en) Pharmaceutical compositions
IN2014MN02106A (en)
WO2012173682A3 (en) Compounds and methods for the treatment of isocitrate dehydrognase related diseases
WO2014043706A8 (en) Method of synthesizing thyroid hormone analogs and polymorphs thereof
HK1203375A1 (en) Method for treating a gd2 positive cancer
SG10201808624VA (en) Polymorphs of selinexor
WO2012099942A3 (en) Methods and compositions for treating metabolic syndrome
IN2014MN01521A (en)
WO2012138147A3 (en) 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof
WO2013098836A8 (en) A bis-quinophthalone pigment and a process for preparing the same
WO2013014665A8 (en) Intermediate compounds and process for the preparation of lurasidone and salts thereof
WO2012117357A3 (en) Process for preparation of ketolide intermediates
WO2013111163A3 (en) Process for the preparation of dabigatran etexilate mesylate and polymorphs of intermediates thereof
WO2014013506A8 (en) Process for production of crystalline xylitol using pichia caribbica and its application for quorum sensing inhibition
HK1209105A1 (en) Vegfr3 inhibitors
WO2013190455A3 (en) Process for the preparation of lurasidone hydrochloride
TN2012000418A1 (en) Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
HK1209104A1 (en) Vegfr3 inhibitors
WO2014003203A3 (en) Method for producing stereoselective epoxyketone compound
MY164880A (en) Process for the preparation of isoxazolyl-methoxy-nicotinic acids
WO2014068333A3 (en) New process
WO2015000900A3 (en) Organic compounds
GB2523674A (en) Compounds as inhibitor of DNA double-strand break repair, methods and applications thereof
MX338556B (en) Methods of isolating 4-chloro-2-fluoro-3-substituted-phenylboroni c acids.

Legal Events

Date Code Title Description
122 Ep: pct application non-entry in european phase

Ref document number: 13836773

Country of ref document: EP

Kind code of ref document: A2