191330-56-0Relevant articles and documents
Preparation method of ezetimibe and key intermediates thereof of lipid-lowering drugs
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, (2017/09/13)
The invention relates to a preparation method of ezetimibe and key intermediates thereof of lipid-lowering drugs. The preparation method is applicable to industrial production.
Intermediate compound of ezetimibe
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Paragraph 0065; 0074; 0075; 0076; 0086; 0097; 0108; 0119, (2018/04/02)
The invention provides a novel intermediate compound of ezetimibe and a preparation method thereof. The preparation method comprises a step of converting 4-(4-fluoro-benzoyl)-butyric acid into 4-[2-(4-fluoro-phenyl)-[1,3]dithiolan-2-yl]-butyric acid by using an unseparated intermediate compound. The method provided by the invention is simple in route, low in price and high in efficiency; and in order to better protect functional groups, the method employs the selectively removable protective group, so the method has the advantages of few impurities, high product purity and high product yield.
Method for preparing ezetimibe degradation impurities
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Paragraph 0050; 0051, (2018/03/24)
The invention discloses a method for preparing ezetimibe degradation impurities, namely, ring-opened impurities and ketone impurities. According to the method, the ring-opened impurities and the ketone impurities are obtained from ezetimibe through alkali reaction or oxidation reaction respectively. The method is easy to operate, mild in reaction and higher in yield, product purity is high, environmental pollution is effectively reduced, the impurities are suitable for impurity spectrum analysis of the raw material medicine and preparations of ezetimibe and can be used as a reference substance of correlated substances to detect the content of degradation products in ezetimibe and the preparations of ezetimibe, and guarantee is provided for further control of product quality of ezetimibe and the preparations of ezetimibe.