发明名称 METHOD FOR SEPARATING DIASTEREOISOMER A OF BEDAQUILINE
摘要 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%.
申请公布号 WO2017015793(A1) 申请公布日期 2017.02.02
申请号 WO2015CN85075 申请日期 2015.07.24
申请人 ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.;SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY 发明人 ZHANG, Fuli;PAN, Linyu;ZHU, Jinjin;WANG, Xinzeng;ZHAO, Li;REN, Zhong;SONG, Ying
分类号 C07D215/227;C07F1/02 主分类号 C07D215/227
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