Title:
PREPARATION METHOD FOR EPLERENONE
Document Type and Number:
WIPO Patent Application WO/2010/118560
Kind Code:
A1
Abstract:
The invention provides a process for preparing eplerenone, which comprises the following steps: (1) in the presence of a side reaction inhibitor, 17α-hydroxyl-3-oxo-γ-lactone-pregn-4,9(11)-diene-7α,21-dicarboxylic acid methyl ester IV is selectively expoxidized on double bond in trichloroacetonitrile, oxidant and phosphate buffer system in solution, to prepare crude eplerenone; (2) the crude eplerenone is recrystallized to yield pure eplerenone. High pure eplerenone can be obtained by the method of the present invention, the purity of eplerenone can reach 99.5% and the yield is as high as 87%. The method of the present invention is suitable for production on an industrial scale.
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Inventors:
CHU DINGJUN (CN)
HONG XIANGXIAN (CN)
HONG XIANGXIAN (CN)
Application Number:
PCT/CN2009/000531
Publication Date:
October 21, 2010
Filing Date:
May 18, 2009
Export Citation:
Assignee:
ZHEJIANG TIANTAI AURISCO PHARM (CN)
SHANGAI AURISCO INTERNAT TRADI (CN)
CHU DINGJUN (CN)
HONG XIANGXIAN (CN)
SHANGAI AURISCO INTERNAT TRADI (CN)
CHU DINGJUN (CN)
HONG XIANGXIAN (CN)
International Classes:
C07J21/00
Foreign References:
| US20080234478A1 | 2008-09-25 | |||
| US4559332A | 1985-12-17 | |||
| CN101318986A | 2008-12-10 |
Attorney, Agent or Firm:
SHANGAI XIN TIAN PATENT AGENT CO., LTD. (No. 59 Nanchang Road, Shanghai 0, CN)
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