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1. IN1798/MUM/2008 - IMPROVED PROCESS FOR SITAGLIPTIN

Office
India
Application Number 1798/MUM/2008
Application Date 27.08.2008
Publication Number 1798/MUM/2008
Publication Date 30.07.2010
Grant Number 271643
Grant Date 04.03.2016
Publication Kind B
IPC
C07C 22/34
C07C 22/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
22Cyclic compounds containing halogen atoms bound to an acyclic carbon atom
Applicants CADILA HEALTHCARE LIMITED
Inventors KOTHARI, HIMANSHU M
DAVE, MAYANK GHANSHYAMBHAI
PANDEY, BIPIN
Title
(EN) IMPROVED PROCESS FOR SITAGLIPTIN
Abstract
(EN) The present invention relates to synthesis of [3-amino acid derivatives and its salts of formula by a novel process. The process comprises the reduction of a protected or unprotected prochiral (3-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic [3- amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4- oxo-4-[3-(trifluoromethyl)-5,6-dihydro[ 1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]- l -(2,4,5- trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms, phosphate": salt and also a Dibenzoyl-L-tartaric acid salt.
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