METHOD FOR RESOLUTION OF CITALOPRAM INTERMEDIATE 5-CYANOGEN DIOL

Title:

METHOD FOR RESOLUTION OF CITALOPRAM INTERMEDIATE 5-CYANOGEN DIOL

Document Type and Number:

WIPO Patent Application WO/2016/074225

Kind Code:

A1

Abstract:

Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl cyanophenyl as an enantiomer thereof, comprising the following steps: crystallizing, in a resolving solvent, a salt formed from (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl cyanophenyl and a resolving agent D-(+)di-p-toluoyl tartaric acid; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.

Inventors:

LIANG ZUNJUN (CN)
HU SIQI (CN)
PENG CAIHUA (CN)
HUANG WENFENG (CN)
LU QIFENG (CN)
TU GUOLIANG (CN)

Application Number:

PCT/CN2014/091139

Publication Date:

May 19, 2016

Filing Date:

November 14, 2014

Export Citation:

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Assignee:

ZHEJIANG HUAHAI PHARM CO LTD (CN)

International Classes:

C07C255/59; C07C253/34

Domestic Patent References:

WO2010004575A2	2010-01-14
WO2006106531A1	2006-10-12
WO2007012954A1	2007-02-01

Foreign References:

CN101386583A	2009-03-18
CN101265215A	2008-09-17
CN102190600A	2011-09-21

Other References: