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:
Jan. 12, 2016

Filed:

Aug. 08, 2013
Applicant:

Cipla Limited, Mumbai, IN;

Inventors:

Dharmaraj Ramachandra Rao, Thane (West) Maharashtra, IN;

Rajendra Narayanrao Kankan, Mumbai Maharashtra, IN;

Maruti Ghagare, Thane (West) Maharashtra, IN;

Swati Atul Kadam, Thane Maharashtra, IN;

Assignee:

CIPLA Limited, Mumbai, IN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 487/04 (2006.01);
U.S. Cl.
CPC ...
C07D 487/04 (2013.01);
Abstract

There is provided a process for the preparation of sitagliptin or a pharmaceutically acceptable salt thereof, and a process for the preparation of intermediate compounds useful in the preparation of sitagliptin. In particular, there is provided a process comprising condensing 3-tert-butoxycarbonylamino-4-(2,4,5-trifluorophenyl)butyric acid of formula (II) with 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine of formula (III) or a salt thereof in presence of a catalyst to obtain (R)-tert-butyl-4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-yl-carbamate of formula (IV) or a pharmaceutically acceptable salt thereof. The catalyst is represented by the compound of formula (V). Compound of formula (IV) or its pharmaceutically acceptable salt obtained may be deprotected to obtain a compound of formula (I).


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