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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.

Inventors:
CHU, Dingjun (No.22, Fengze Rd.Tiantai, Zhejiang 0, 317200, CN)
褚定军 (中国浙江省天台县城关丰泽路22号, Zhejiang 0, 317200, CN)
Application Number:
CN2009/000531
Publication Date:
October 21, 2010
Filing Date:
May 18, 2009
Export Citation:
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Assignee:
ZHEJIANG TIANTAI AURISCO PHARMACEUTICAL CO., LTD. (No.22, Fengze Rd.Tiantai, Zhejiang 0, 317200, CN)
浙江省天台县奥锐特药业有限公司 (中国浙江省天台县城关丰泽路22号, Zhejiang 0, 317200, CN)
SHANGAI AURISCO INTERNATIONAL TRADING CO., LTD. (Rm 1709∼1710, Hitech PlazaNo.488, South Wuning Road,Jing'an District, Shanghai 2, 200042, CN)
上海奥锐特国际贸易有限公司 (中国上海市静安区武宁南路488号智慧广场1709-1710室, Shanghai 2, 200042, CN)
International Classes:
C07J21/00
Foreign References:
US20080234478A1
US4559332A
CN101318986A
Attorney, Agent or Firm:
SHANGAI XIN TIAN PATENT AGENT CO., LTD. (Rm. 1606, No. 59 Nanchang Road, Shanghai 0, 200020, CN)
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