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Title:
METHOD FOR SEPARATING DIASTEREOISOMER A OF BEDAQUILINE
Document Type and Number:
WIPO Patent Application WO/2017/015793
Kind Code:
A1
Abstract:
Disclosed is a method for separating a diastereoisomer A of Bedaquiline. The method comprises the following steps: (1) adding a reversed-phase solvent into a Bedaquiline reaction liquid comprising diastereoisomers A and B, so as to precipitate out the diastereoisomer B; and (2) removing the diastereoisomer B precipitated out in step (1), so as to obtain the diastereoisomer A. The separation method of the present invention is easy to operate and is stable, and has higher industrialization value compared with separation and purification in a conventional column chromatography method, and can resolve the problems of difficulty in purifying and separating Bedaquiline due to the small amount of a product caused by an excessively low conversion rate because preparation condition of Bedaquiline is harsh and the conversion rate is difficult to ensure; raw material residuals can be easily removed, the yield is high, and the purity of the diastereoisomer A is high, which facilitates the split; split can be further carried out to obtain a qualified Bedaquiline product with a purity greater than or equal to 99.0%, wherein the impurities of the diastereoisomers are lower than or equal to 0.1%.

Inventors:
ZHANG, Fuli (No.1320, West Beijing Road Jing'an District, Shanghai 0, 200040, CN)
PAN, Linyu (No.1320, West Beijing Road Jing'an District, Shanghai 0, 200040, CN)
ZHU, Jinjin (No.1320, West Beijing Road Jing'an District, Shanghai 0, 200040, CN)
WANG, Xinzeng (No. 46 Waisha Road, Jiaojiang DistrictTaizhou, Zhejiang 0, 318000, CN)
ZHAO, Li (No. 46 Waisha Road, Jiaojiang DistrictTaizhou, Zhejiang 0, 318000, CN)
REN, Zhong (No. 46 Waisha Road, Jiaojiang DistrictTaizhou, Zhejiang 0, 318000, CN)
SONG, Ying (No. 46 Waisha Road, Jiaojiang DistrictTaizhou, Zhejiang 0, 318000, CN)
Application Number:
CN2015/085075
Publication Date:
February 02, 2017
Filing Date:
July 24, 2015
Export Citation:
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Assignee:
ZHEJIANG HISUN PHARMACEUTICAL CO., LTD. (No. 46 Waisha Road, Jiaojiang DistrictTaizhou, Zhejiang 0, 318000, CN)
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (No.1320 West Beijing Road, Jing'an District, Shanghai 0, 200040, CN)
International Classes:
C07D215/227; C07F1/02
Foreign References:
CN101180302A2008-05-14
Attorney, Agent or Firm:
BOSS & YOUNG PATENT AND TRADEMARK LAW OFFICE et al. (5/F, Tower A Bldg. No. 1, GT International Center,Jia 3 Yongandongli, Jianguomenwai Avenue,Chaoyang District, Beijing 2, 100022, CN)
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