Method for preparing rosuvastatin calcium

A technology for rosuvastatin and compounds, which is applied in the field of pharmaceutical preparation, can solve the problems of expensive reagents, harsh reaction conditions and the like, and achieves the effects of stable yield, easy operation and low price
CN102219749BActive Publication Date: 2013-07-17ZHEJIANG JINGXIN PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG JINGXIN PHARMA
Publication Date
2013-07-17

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Abstract

The invention provides a preparation method of rosuvastatin calcium. The method comprises the following steps: carrying out condensation reaction on 4-(4-fluorophenyl)-6-isopropyl-2 chloropyrimidine-5-formaldehyde and (3R)-tertiary butyl dimethylsiloxo-5-oxo-6-triphenyl phosphaalkene hexanoate; and then removing a silylether protecting group of hydroxyl, carrying out stereoselectivity reduction, reacting with 2,2-dimethoxy propane, condensing with N-methyl methane sulfonamide, removing propylidene protection, hydrolyzing an ester group, salifying and carrying out other steps, so as to obtain the rosuvastatin calcium. According to the preparation method, the yield is stable, and the price of reagents is cheap; and the method is easy to operate and is beneficial to industrial production.
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Description

technical field

[0001] The invention relates to medicine preparation, in particular to a preparation method of rosuvastatin calcium. Background technique

[0002] The chemical name of rosuvastatin calcium is: (+)-(3R,5S)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methyl Calcium sulfonylamino)pyrimidin-5-yl]-3,5-dihydroxy-6-(E)-heptenoate. The chemical structural formula is:

[0003]

[0004] Rosuvastatin was successfully developed by Shionogi Company of Japan (Osaka Shionogi Company), and was transferred to AstraZeneca Company for development and marketed worldwide. Rosuvastatin has been widely used as a prescription drug for blood lipid regulation due to its satisfactory clinical results in terms of efficacy and safety.

[0005] The preparation process of rosuvastatin calcium has been reported in numerous documents and patents, such as the method reported in the document (Bioorganic & MedicinalChemistry.vol.5.NO.2.pp.437-444.1997,), the important intermediate 4- ...

Claims

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