WO2014020555A3 - Improved process for preparing dabigatran etexilate mesylate - Google Patents

Improved process for preparing dabigatran etexilate mesylate Download PDF

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Publication number
WO2014020555A3
WO2014020555A3 PCT/IB2013/056288 IB2013056288W WO2014020555A3 WO 2014020555 A3 WO2014020555 A3 WO 2014020555A3 IB 2013056288 W IB2013056288 W IB 2013056288W WO 2014020555 A3 WO2014020555 A3 WO 2014020555A3
Authority
WO
WIPO (PCT)
Prior art keywords
dabigatran etexilate
etexilate mesylate
improved process
preparing
preparing dabigatran
Prior art date
Application number
PCT/IB2013/056288
Other languages
French (fr)
Other versions
WO2014020555A2 (en
Inventor
Venkat Raman JAYARAMAN
Samir Patel
Samir Mistry
Mukesh Timbadiya
Bhupendra Parmar
Jignesh Patel
Original Assignee
Alembic Pharmaceuticals 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 Alembic Pharmaceuticals Limited filed Critical Alembic Pharmaceuticals Limited
Publication of WO2014020555A2 publication Critical patent/WO2014020555A2/en
Publication of WO2014020555A3 publication Critical patent/WO2014020555A3/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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

An improved process for preparing 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl- carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide methanesulfonate salt (dabigatran etexilate mesylate) and a process for purifying dabigatran etexilate mesylate are provided. Further, a process for preparing an intermediate of dabigatran etexilate mesylate of formula (VI) is provided.
PCT/IB2013/056288 2012-08-01 2013-07-31 An improved process for the preparation of dabigatran etexilate mesylate WO2014020555A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2215/MUM/2012 2012-08-01
IN2215MU2012 2012-08-01

Publications (2)

Publication Number Publication Date
WO2014020555A2 WO2014020555A2 (en) 2014-02-06
WO2014020555A3 true WO2014020555A3 (en) 2014-03-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2013/056288 WO2014020555A2 (en) 2012-08-01 2013-07-31 An improved process for the preparation of dabigatran etexilate mesylate

Country Status (1)

Country Link
WO (1) WO2014020555A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN104725360A (en) * 2015-04-09 2015-06-24 重庆东得医药科技有限公司 Preparing method of dabigatran etexilate mesylate crystal form I
CN104892576A (en) * 2015-05-27 2015-09-09 上海应用技术学院 Purification method for Dabigatran etexilate analogue intermediate
CN105037253A (en) * 2015-05-27 2015-11-11 上海应用技术学院 Method for purifying compound through ultrasonic crystal precipitation
CN105294651A (en) * 2015-09-23 2016-02-03 烟台东诚药业集团股份有限公司 Method for synthesizing and preparing pradaxa formamidine intermediates
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
CN107686476A (en) * 2017-09-04 2018-02-13 扬子江药业集团广州海瑞药业有限公司 A kind of preparation technology of dabigatran etexilate methanesulfonate
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7202368B2 (en) * 2004-06-25 2007-04-10 Boehringer Ingelheim International Gmbh Process for the preparation of 4-(benzimidazolymethylamino) benzamidines
WO2012004396A2 (en) * 2010-07-09 2012-01-12 Esteve Química, S.A. Process of preparing a thrombin specific inhibitor
WO2012027543A1 (en) * 2010-08-25 2012-03-01 Teva Pharmaceuticals Usa, Inc. Solid state forms of dabigatran etexilate, dabigatran etexilate mesylate and processes for preparation thereof
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts
WO2013150545A2 (en) * 2012-04-02 2013-10-10 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and salts thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7202368B2 (en) * 2004-06-25 2007-04-10 Boehringer Ingelheim International Gmbh Process for the preparation of 4-(benzimidazolymethylamino) benzamidines
WO2012004396A2 (en) * 2010-07-09 2012-01-12 Esteve Química, S.A. Process of preparing a thrombin specific inhibitor
WO2012027543A1 (en) * 2010-08-25 2012-03-01 Teva Pharmaceuticals Usa, Inc. Solid state forms of dabigatran etexilate, dabigatran etexilate mesylate and processes for preparation thereof
WO2012077136A2 (en) * 2010-12-06 2012-06-14 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and its salts
WO2013150545A2 (en) * 2012-04-02 2013-10-10 Msn Laboratories Limited Process for the preparation of benzimidazole derivatives and salts thereof

Also Published As

Publication number Publication date
WO2014020555A2 (en) 2014-02-06

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