METHOD FOR PREPARING CITALOPRAM GLYCOL INTERMEDIATE

Title:

METHOD FOR PREPARING CITALOPRAM GLYCOL INTERMEDIATE

Document Type and Number:

WIPO Patent Application WO/2016/197320

Kind Code:

A1

Abstract:

The present invention relates to a method for preparing a Citalopram glycol intermediate represented by formula IV. The method comprises the following steps: in the existence of an auxiliary reagent metal salt, allowing 5-cyanophthalide to sequentially subjected to a Grignard addition reaction with fluoropheny magnesium halide and N, N-dimethyl amino propyl magnesium halide in an organic solvent; and after the reaction is completed, performing hydrolysis and decomposition to obtain a Citalopram glycol intermediate represented by formula IV. In the present invention, by adding an auxiliary reagent metal salt, the activity and the selectivity of a Grignard reaction are remarkably improved, and the reaction yield is obviously enhanced.

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Inventors:

LIANG ZUNJUN (CN)
XIAO WEIFENG (CN)
PENG CAIHUA (CN)
HUANG WENFENG (CN)
TU GUOLIANG (CN)

Application Number:

PCT/CN2015/081054

Publication Date:

December 15, 2016

Filing Date:

June 09, 2015

Export Citation:

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Assignee:

ZHEJIANG HUAHAI PHARM CO LTD (CN)

International Classes:

C07C255/59; C07C253/30

Domestic Patent References:

WO2006106531A1

2006-10-12

Foreign References:

CN102675152A	2012-09-19
CN104072390A	2014-10-01

Other References: