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Title:
METHOD FOR PREPARING ZYTIGA INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2015/188791
Kind Code:
A1
Abstract:
Disclosed is a method for preparing a Zytiga intermediate. The intermediate is trifluoromethanesulfonate of dehydroepiandrosterone acetate and has a chemical structure represented by formula (II). In the method, dehydroepiandrosterone acetate and trifluoromethanesulfonic anhydride are subjected to sulfonylation reaction in a weak-base condition, and the weak-base condition is formed by at least one base of C1-C4 carboxylate of alkaline metal, C1-C4 carboxylate of alkaline-earth metal, oxalate of alkaline metal, oxalate of alkaline-earth metal, hydrophosphate of alkaline metal, hydrophosphate of alkaline-earth metal, fluoride of alkaline metal and fluoride of alkaline-earth metal. The present invention has advantages of environmental friendliness, mild reaction condition, simple operation and few side reactions, and facilitates industrialized mass production.

Inventors:
AN XIAOXIA (CN)
MAO FENGWANG (CN)
ZHAO JIANGYONG (CN)
HUANG CHENGJUN (CN)
Application Number:
PCT/CN2015/081490
Publication Date:
December 17, 2015
Filing Date:
June 15, 2015
Export Citation:
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Assignee:
JIANGSU CDYMAX PHARMACEUTICALS CO LTD (CN)
SHANGHAI ACEBRIGHT PHARMACEUTICALS GROUP CO LTD (CN)
International Classes:
C07J31/00; C07J43/00
Foreign References:
CN103193849A2013-07-10
CN101044155A2007-09-26
Other References:
ANONYMOUSLY: "Preparation of Enol-Triflate in the Presence of Inorganic Bases", IP.COM JOURNAL, vol. 13, no. 3A, 19 February 2013 (2013-02-19), XP055244410, ISSN: 1533-0001
Attorney, Agent or Firm:
XU & PARTNERS,LLC. (CN)
上海一平知识产权代理有限公司 (CN)
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