Title:
METHOD FOR PURIFYING KEY INTERMEDIATES OF CITALOPRAM
Document Type and Number:
WIPO Patent Application WO/2022/151968
Kind Code:
A1
Abstract:
The present invention relates to a method for purifying key intermediates of Citalopram, i.e. 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile and a salt thereof. The method comprises dissolving crude 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile (compound of formula I containing formaldehyde impurity) with an organic solvent, adding a washing solution, controlling the temperature, stirring, leaving to stand for layering, and removing the aqueous layer, so as to obtain a purified organic solution of 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile. The method provided by the present invention can effectively remove aldehyde group-containing impurities in the intermediate. The method of the present invention has the advantages of simple operation, cheap raw materials and mild conditions, and is suitable for large-scale industrial production.
Inventors:
ZHANG JIAN (CN)
WANG JICHAO (CN)
YOU XIANGQIAN (CN)
QIAN LIANGWEI (CN)
ZHOU TAO (CN)
HU JIAXING (CN)
HUANG WENFENG (CN)
WANG JICHAO (CN)
YOU XIANGQIAN (CN)
QIAN LIANGWEI (CN)
ZHOU TAO (CN)
HU JIAXING (CN)
HUANG WENFENG (CN)
Application Number:
PCT/CN2021/141912
Publication Date:
July 21, 2022
Filing Date:
December 28, 2021
Export Citation:
Assignee:
ZHEJIANG HUAHAI PHARM CO LTD (CN)
ZHEJIANG HUAHAI LICHENG PHARMACEUTICAL CO LTD (CN)
ZHEJIANG HUAHAI LICHENG PHARMACEUTICAL CO LTD (CN)
International Classes:
C07C253/30; C07C255/59
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Other References:
YANG HONGKUN, ET AL.: "Synthesis of a Related Substance of Escitalopram", CHINESE JOURNAL OF MEDICINAL CHEMISTRY, GAI-KAI BIANJIBU, CN, vol. 25, no. 5, 31 October 2015 (2015-10-31), CN , pages 389 - 392, XP055950164, ISSN: 1005-0108, DOI: 10.14142/j.cnki.cn21-1313/r.2015.05.011
Attorney, Agent or Firm:
PATENTSINO IP FIRM (CN)
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