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Title:
NEW VORTIOXETINE INTERMEDIATE AND SYNTHESIS PROCESS THEREOF
Document Type and Number:
WIPO Patent Application WO/2015/169130
Kind Code:
A1
Abstract:
Provided in the present invention are a new intermediate II and a synthesis process thereof, the synthesis process comprising: (a) using a compound of formula I as a raw material, the intermediate II is obtained by diazo reaction, followed by halogenating reaction; and (b) the intermediate II is reacted with a compound III, so as to obtain a compound IV which is hydrolyzed without separation to obtain vortioxetine as shown in compound V. The intermediate II can be used for synthesizing vortioxetine.

Inventors:
TANG CAIDE (CN)
WANG GANG (CN)
WANG BOYU (CN)
HUANG LUNING (CN)
GU ERIC (CN)
Application Number:
PCT/CN2015/075018
Publication Date:
November 12, 2015
Filing Date:
March 25, 2015
Export Citation:
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Assignee:
SHANGHAI SYNCORES TECHNOLOGIES INC LTD (CN)
ZHEJIANG HUAHAI PHARM CO LTD (CN)
International Classes:
C07D295/096; C07D295/205; C07D295/185
Domestic Patent References:
WO2011072174A12011-06-16
Foreign References:
EP0548798A11993-06-30
CN1541214A2004-10-27
Other References:
BANG-ANDERSEN, BENNY ET AL.: "Discovery of 1-[2-(2,4-Dimethylphenylsulfanyl) phenyl] piperazine (Lu AA21004): A Novel Multimodal Compound for the Treatment of Major Depressive Disorder", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 9, 12 April 2011 (2011-04-12), pages 3206 - 3221, XP055058222, ISSN: 0022-2623
ANDERSEN, VALDEMAR L. ET AL.: "11C-labeling and preliminary evaluation of vortioxetine as a PET radioligand", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 24, no. 11, 19 April 2014 (2014-04-19), pages 2408 - 2411, XP028660040, ISSN: 0960-894x
BANG-ANDERSEN, BENNY ET AL.: "Discovery of 1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A Novel Multimodal Compound for the Treatment of Major Depressive Disorder", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 9, 12 April 2011 (2011-04-12), pages 3206 - 3221, XP055058222, ISSN: 0022-2623
KRAFFT, EVA A. ET AL.: "An improved synthesis of Lu AA20465", TETRAHEDRON LETTERS, vol. 47, no. 30, 9 June 2006 (2006-06-09), pages 5355 - 5357, XP025004533, ISSN: 0040-4039
See also references of EP 3141543A4
Attorney, Agent or Firm:
PATENTSINO IP FIRM (CN)
北京柏杉松知识产权代理事务所(普通合伙) (CN)
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