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1. (WO2017060924) A NOVEL PIPECOLIC ACID CO-CRYSTAL OF CANAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF

Pub. No.:    WO/2017/060924    International Application No.:    PCT/IN2016/050344
Publication Date: Fri Apr 14 01:59:59 CEST 2017 International Filing Date: Sun Oct 09 01:59:59 CEST 2016
IPC: C07D 409/10
Applicants: HARMAN FINOCHEM LIMITED
Inventors: KADAM, Vijay Trimbak
SAIKRISHNA, ,
BHOSLE, Shrikrushna Ramrao
MINHAS, Harpreet Singh
MINHAS, Gurpreet Singh
Title: A NOVEL PIPECOLIC ACID CO-CRYSTAL OF CANAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF
Abstract:
The present invention discloses the process for preparation of (2S,3R,4R,5S,6R)- 2-{3-[5-[4-Fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-6- hydroxymethyl-tetrahydro-pyran-3,4,5-triol and its pipecolic acid co-crystal. The invention also discloses novel intermediate, acetic acid 4, 5-diacetoxy-6- acetoxymethyl-2-R1-2-{3-[5-(4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl- phenyl}-tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl, as an intermediate for the preparation of 4, 5-diacetoxy-6-acetoxymethyl-2-R1-2-{3-[5- (4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl.