A method for separating bedaquiline diastereomer a

A technology of diastereoisomers and bedaquiline, applied in the field of separation of bedaquiline diastereomer A, can solve the problem of low purity of diastereomer A and difficult control of reaction conditions , Inability to purify and separate products, etc., to achieve high purity and yield, high purity, and the effect of easy raw material residue
CN107848978BActive Publication Date: 2021-04-02ZHEJIANG HISUN PHARMA CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG HISUN PHARMA CO LTD
Publication Date
2021-04-02

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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%.
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Description

technical field

[0001] The invention relates to the field of medicines, more specifically, to a method for separating bedaquiline diastereoisomer A. Background technique

[0002] Bedaquiline (Bedaquiline) is a kind of anti-tuberculosis drug, and its structural formula is as shown in 1:

[0003]

[0004] The chemical name of bedaquiline is (1R,2S)-1-(6-bromo-2-methoxy-3-quinolyl)-4-dimethylamino-2-(1-naphthyl)-1 -Phenyl-2-butanol is the first drug that inhibits mycobacterial adenosine triphosphate (ATP) synthetase developed by Johnson & Johnson. The trade name is Sirturo. Bedaquiline has strong selectivity to ATP synthase of Mycobacterium tuberculosis, and its new mechanism of action makes it have no cross-resistance with other anti-tuberculosis drugs, which will greatly reduce the drug resistance of Mycobacterium tuberculosis. It showed good activity against multidrug-resistant tuberculosis bacteria in macrophages, suggesting that it has the effect of shortening the tr...

Claims

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