WO2015124764A8 - Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate - Google Patents

Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate Download PDF

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Publication number
WO2015124764A8
WO2015124764A8 PCT/EP2015/053702 EP2015053702W WO2015124764A8 WO 2015124764 A8 WO2015124764 A8 WO 2015124764A8 EP 2015053702 W EP2015053702 W EP 2015053702W WO 2015124764 A8 WO2015124764 A8 WO 2015124764A8
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WO
WIPO (PCT)
Prior art keywords
dabigatran etexilate
intermediates
mesylate
novel polymorph
synthesis process
Prior art date
Application number
PCT/EP2015/053702
Other languages
French (fr)
Other versions
WO2015124764A1 (en
Inventor
Massimo Ferrari
Daniele DE ZANI
Maurizio Valentincic
Original Assignee
Erregierre S.P.A.
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 Erregierre S.P.A. filed Critical Erregierre S.P.A.
Publication of WO2015124764A1 publication Critical patent/WO2015124764A1/en
Publication of WO2015124764A8 publication Critical patent/WO2015124764A8/en

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    • 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)

Abstract

A novel process is described for the production of Dabigatran etexilate mesylate, a compound having the following structural formula and two novel intermediates of said process.
PCT/EP2015/053702 2014-02-24 2015-02-23 Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate WO2015124764A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI20140272 2014-02-24
ITMI2014A000272 2014-02-24

Publications (2)

Publication Number Publication Date
WO2015124764A1 WO2015124764A1 (en) 2015-08-27
WO2015124764A8 true WO2015124764A8 (en) 2015-12-30

Family

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PCT/EP2015/053702 WO2015124764A1 (en) 2014-02-24 2015-02-23 Synthesis process of dabigatran etexilate mesylate, intermediates of the process and novel polymorph of dabigatran etexilate

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WO (1) WO2015124764A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017037743A2 (en) * 2015-09-03 2017-03-09 Sun Pharmaceutical Industries Limited Dabigatran etexilate 1,4-butanedisulfonate salt and its crystal form
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
CN105153118A (en) * 2015-09-24 2015-12-16 青岛黄海制药有限责任公司 Central control method of midbody in dabigatran etexilate mesylate preparation process
CN105906607A (en) * 2015-12-23 2016-08-31 嘉实（湖南）医药科技有限公司 Dabigatran etexilate synthesis method
CN108658939B (en) * 2018-07-16 2021-07-20 上海现代制药股份有限公司 Synthesis method of dabigatran etexilate mesylate key intermediate
CN115141124A (en) * 2022-06-16 2022-10-04 重庆华森制药股份有限公司 Method for preparing gabexate mesylate

Family Cites Families (16)

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US6087380A (en) 1949-11-24 2000-07-11 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions
DE102005020002A1 (en) 2005-04-27 2006-11-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg New hexyloxycarbonylamino-imino-methyl-phenylamino-methyl-benzimidazole-pyridine-propionic acid-ethyl ester salts such as hydrochloride useful for the prophylaxis of vein thrombosis and stroke
DE102005025728A1 (en) 2005-06-04 2006-12-07 Boehringer Ingelheim Pharma Gmbh & Co. Kg Polymorphs of 3 - [(2 - {[4- (hexyloxycarbonylamino-imino-methyl) -phenyl-amino] -methyl} -1-methyl-1H-benzimidazole-5-carbonyl) -pyridin-2-yl-amino] -propionic acid ethyl ester
JP2010505906A (en) 2006-10-10 2010-02-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 3-[(2-{[4- (Hexyloxycarbonylamino-imino-methyl) -phenylamino] -methyl} -1-methyl-1H-benzimidazol-5-carbonyl) -pyridin-2-yl-amino] -Physiologically acceptable salt of propionic acid ethyl ester
DE102006054005A1 (en) 2006-11-16 2008-05-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg New polymorphs of 3 - [(2 - {[4- (hexyloxycarbonylamino-imino-methyl) -phenyl-amino] -methyl} -1-methyl-1H-benzimidazole-5-carbonyl) -pyridin-2-yl-amino] -propionic acid ethyl
CZ305085B6 (en) * 2008-03-14 2015-04-29 Zentiva, K.S. Process for preparing dabigatran
CN102985416B (en) * 2010-07-09 2015-04-01 埃斯特维化学股份有限公司 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
HUE026408T2 (en) 2010-09-27 2016-06-28 Ratiopharm Gmbh Dabigatran etexilate bismesylate salt, solid state forms and process for preparation thereof
US9006448B2 (en) 2010-12-06 2015-04-14 Msn Laboratories Private Limited Process for the preparation of benzimidazole derivatives and its salts
EP2522662A1 (en) * 2011-05-11 2012-11-14 Medichem, S.A. Dabigatran etexilate and related substances, processes and compositions, and use of the substances as reference standards and markers
US9212166B2 (en) 2012-01-20 2015-12-15 Cadila Healthcare Limited Process for the preparation of dabigatran etexilate mesylate and polymorphs of intermediates thereof
WO2013124749A1 (en) 2012-02-20 2013-08-29 Alembic Pharmaceuticals Limited Novel polymorph of dabigatran etexilate
EP2631234A1 (en) 2012-02-23 2013-08-28 Esteve Química, S.A. Solid forms of dabigatran etexilate mesylate and processes for their preparation
WO2013144903A1 (en) 2012-03-28 2013-10-03 Dr. Reddy's Laboratories Limited Processes for the preparation of dabigatran etexilate
US9273030B2 (en) * 2012-04-02 2016-03-01 Msn Laboratories Private Limited Process for the preparation of benzimidazole derivatives and salts thereof

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WO2015124764A1 (en) 2015-08-27

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