Invention Grant
- Patent Title: Method for the preparation of dabigatran
- Patent Title (中): 达比加群的制备方法
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Application No.: US12922214Application Date: 2009-03-10
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Publication No.: US08394961B2Publication Date: 2013-03-12
- Inventor: Josef Jirman , Jindrich Richter , Petr Lustig
- Applicant: Josef Jirman , Jindrich Richter , Petr Lustig
- Applicant Address: CZ Praha
- Assignee: Zentiva k.s.
- Current Assignee: Zentiva k.s.
- Current Assignee Address: CZ Praha
- Agency: Pearl Cohen Zedek Latzer, LLP
- Priority: CZ2008-165 20080314
- International Application: PCT/CZ2009/000037 WO 20090310
- International Announcement: WO2009/111997 WO 20090917
- Main IPC: C07D401/12
- IPC: C07D401/12

Abstract:
A method for the manufacture of dabigatran of formula VIII, in which the product of a reaction of 4-ethylamino-3-nitrobenzoic acid chloride with ethyl-3-(pyridin-2-ylamino)propanoate, is converted to the hydrochloride using a hydrogen chloride solution producing the compound of formula III-HCl, in which the nitro group is reduced by means of a reaction with sodium dithionite, and the resulting compound of formula IV is subjected to a reaction with [(4-cyanophenyl)amino]acetic acid and oxalic acid, the product of this reaction VI-oxal is then subjected to hydrolysis and a reaction with ammonium carbonate to produce the intermediate of formula VII-HCl, which is then converted to dabigatran by means of a reaction with hexyl chloroformate.
Public/Granted literature
- US20110082299A1 METHOD FOR THE PREPARATION OF DABIGATRAN Public/Granted day:2011-04-07
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