The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 12, 2013

Filed:

Mar. 10, 2009
Applicants:

Josef Jirman, Praha, CZ;

Jindrich Richter, Pardubice, CZ;

Petr Lustig, Pardubice, CZ;

Inventors:

Josef Jirman, Praha, CZ;

Jindrich Richter, Pardubice, CZ;

Petr Lustig, Pardubice, CZ;

Assignee:

Zentiva k.s., Praha, CZ;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/12 (2006.01);
U.S. Cl.
CPC ...
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.


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