Title:
NOVEL PREPARATION METHOD FOR CITALOPRAM AND ESCITALOPRAM USING CARBONATES
Document Type and Number:
WIPO Patent Application WO/2020/060011
Kind Code:
A1
Abstract:
The present invention relates to a method for preparing citalopram and escitalopram, and addition salts using same. In the preparation of citalopram and escitalopram, intermediate compounds are not separately obtained before a cyclization process, and 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxy-1-butyl]-3-(hydroxymethyl)benzonitrile represented by chemical formula 3 or (S)-(-)-4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxy-1-butyl]-3-(hydroxymethyl)-benzonitrile represented by chemical formula 3a is cyclized using carbonate compounds without subsequent treatment processes, such as separation and concentration, of intermediate compounds, thereby preparing citalopram and escitalopram with high purity and high yield.
Inventors:
LEE YOUNG-KEUN (KR)
OH YOUNG-SEON (KR)
KIM JUNG-JIN (KR)
CHA YOUNG-NAM (KR)
OH GI-BUM (KR)
OH YOUNG-SEON (KR)
KIM JUNG-JIN (KR)
CHA YOUNG-NAM (KR)
OH GI-BUM (KR)
Application Number:
PCT/KR2019/008035
Publication Date:
March 26, 2020
Filing Date:
July 02, 2019
Export Citation:
Assignee:
UK CHEMIPHARM CO LTD (KR)
International Classes:
C07D307/87; A61K31/343; A61P25/24
Domestic Patent References:
| WO2008059514A2 | 2008-05-22 |
Foreign References:
| JP2018016569A | 2018-02-01 | |||
| KR20170048878A | 2017-05-10 | |||
| US20090099375A1 | 2009-04-16 |
Other References:
ARICO, F.: "Synthesis of five- and six-membered heterocycles by dimethyl carbonate with catalytic amounts of nitrogen bicyclic bases", GREEN CHEMISTRY, 2015, pages 1176 - 1185, XP020193149
Attorney, Agent or Firm:
HANSUNG INTELLECTUAL PROPERTY (KR)
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