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WO2015128875A3 - A process for preparation of dabigatran etexilate mesylate and intermediates thereof - Google Patents

A process for preparation of dabigatran etexilate mesylate and intermediates thereof Download PDF

Info

Publication number
WO2015128875A3
WO2015128875A3 PCT/IN2015/000100 IN2015000100W WO2015128875A3 WO 2015128875 A3 WO2015128875 A3 WO 2015128875A3 IN 2015000100 W IN2015000100 W IN 2015000100W WO 2015128875 A3 WO2015128875 A3 WO 2015128875A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
dabigatran etexilate
intermediates
etexilate mesylate
relates
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/IN2015/000100
Other languages
French (fr)
Other versions
WO2015128875A2 (en
Inventor
Vijayavitthal Thippannachar Mathad
Pavankumar Vrajlal Solanki
Sekhar Babu UPPELLI
Ganesh Gitaram SARODE
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.)
Megafine Pharma P Ltd
Original Assignee
Megafine Pharma P 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 Megafine Pharma P Ltd filed Critical Megafine Pharma P Ltd
Publication of WO2015128875A2 publication Critical patent/WO2015128875A2/en
Publication of WO2015128875A3 publication Critical patent/WO2015128875A3/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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

The present invention relates to an improved process for the preparation of Dabigatran etexilate and its acid addition salts thereof, wherein the said process substantially eliminates the potential impurities. The present invention also relates to an intermediate of Dabigatran etexilate and process for preparation thereof.
PCT/IN2015/000100 2014-02-26 2015-02-23 A process for preparation of dabigatran etexilate mesylate and intermediates thereof Ceased WO2015128875A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN675/MUM/2014 2014-02-26
IN675MU2014 IN2014MU00675A (en) 2014-02-26 2015-02-23

Publications (2)

Publication Number Publication Date
WO2015128875A2 WO2015128875A2 (en) 2015-09-03
WO2015128875A3 true WO2015128875A3 (en) 2015-11-12

Family

ID=53267425

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2015/000100 Ceased WO2015128875A2 (en) 2014-02-26 2015-02-23 A process for preparation of dabigatran etexilate mesylate and intermediates thereof

Country Status (2)

Country Link
IN (1) IN2014MU00675A (en)
WO (1) WO2015128875A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105732433A (en) * 2016-04-13 2016-07-06 山东新华制药股份有限公司 Refining method of Dabigatran etexilate intermediate condensation compound
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
CN111690699A (en) * 2020-05-19 2020-09-22 浙江工业大学 Method for enzymatic on-line synthesis of 3- (pyridine-2-amino) propylhydroxamic acid
CN114113346B (en) * 2020-08-25 2024-01-12 石药集团恩必普药业有限公司 Detection method of ethyl p-toluenesulfonate and isopropyl p-toluenesulfonate in dabigatran etexilate bulk drug or preparation
CN114716411B (en) * 2022-04-29 2024-03-15 天方药业有限公司 Method for recovering and preparing dabigatran etexilate mesylate from production mother liquor
CN115417855A (en) * 2022-09-22 2022-12-02 安徽美诺华药物化学有限公司 Synthesis process of dabigatran etexilate mesylate

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050107409A1 (en) * 2003-03-10 2005-05-19 Boehringer Ingelheim International Gmbh Aromatic bicyclic compounds, preparation thereof and their use as pharmaceutical compositions
US20050234104A1 (en) * 2003-08-29 2005-10-20 Boehringer Ingelheim International Gmbh 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl)phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methansulfonate and its use as medicament
WO2009111997A1 (en) * 2008-03-14 2009-09-17 Zentiva, K.S. A method for the preparation of dabigatran
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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE121699A1 (en) 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma BICYCLE HETERO CYCLES DISSTITUTED AS INHIBITORS OF THROMBIN
EP1609784A1 (en) 2004-06-25 2005-12-28 Boehringer Ingelheim Pharma GmbH & Co.KG Process for the preparation of 4-(benzimidazolylmethylamino)-benzamidines
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
ITTO20050486A1 (en) 2005-07-14 2005-10-13 Dumitru Bucuresteanu AIR OPERATING COMPRESSOR WITH CONTINUOUS PROPELLER IN A TURNTABLE TUBE
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
CZ2008669A3 (en) 2008-10-24 2010-05-05 Zentiva, A. S. Process for preparing dabigatran and intermediates thereof
HUP1100244A2 (en) 2011-05-11 2012-11-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag Pharmaceutical intermediates and process for their production

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050107409A1 (en) * 2003-03-10 2005-05-19 Boehringer Ingelheim International Gmbh Aromatic bicyclic compounds, preparation thereof and their use as pharmaceutical compositions
US20050234104A1 (en) * 2003-08-29 2005-10-20 Boehringer Ingelheim International Gmbh 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl)phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methansulfonate and its use as medicament
WO2009111997A1 (en) * 2008-03-14 2009-09-17 Zentiva, K.S. A method for the preparation of dabigatran
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

Also Published As

Publication number Publication date
IN2014MU00675A (en) 2015-10-23
WO2015128875A2 (en) 2015-09-03

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