Asymchem Laboratories (tianjin) Co., Ltd.

Asymchem Life Science (tianjin) Co., Ltd

Jilin Asymchem Laboratories Co., Ltd.

Asymchem Laboratories (fuxin) Co., Ltd.

Tianjin Asymchem Pharmaceutical Co., Ltd.

Asymchem Life Science Co., Ltd.

Litao Shen

Hao Hong

Jiuyuan Li

Lei Zhang

James Gage

Chaoyong Chen

Changfeng Li

Lina Guo

Changming Dong

Hongying Tian

The present invention relates to a preparation method for a chiral intermediate for use in statins, acquired with chloroacetic acid and benzyl alcohol as starting materials via a series of reactions, namely etherification, condensation, substitution, and asymmetric reduction. The preparation method provided in the present invention has a novel route of synthesis, allows an intermediate compound to be introduced conveniently into the chiral center of a glycol via enzyme reduction, and not only is low in costs, but also is reliable in quality. The route of synthesis provided in the present invention uses raw materials of low costs, has an easy to operate process, and provides a final product of great purity and high yield.

Preparation method for chiral intermediate for use in statins

A method for preparing sulfobutyl ether-&#x3b2;-cyclodextrin. &#x3b2;-cyclodextrin and 1,4-sulfobutyrolactone are used as raw materials, and a proper amount of an organic solvent is introduced into an alkaline aqueous solution, so that the solubility of the 1,4-sulfobutyrolactone is increased, and the synthesis yield of the sulfobutyl ether-&#x3b2;-cyclodextrin is improved. Operations including ultrasonic dialysis, active carbon decoloration, freeze-drying and so on are performed on the obtained product solution, so as to obtain a powder product of the sulfobutyl ether-beta-cyclodextrin.

Method for preparing sulfobutyl ether-&#x3b2;-cyclodextrin

Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost. 

Intermediate compound for preparing rosuvastatin calcium and method for preparing rosuvastatin calcium therefrom

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Litao Shen