1094100-06-7Relevant articles and documents
Synthesis method of chiral isomer impurities of rosuvastatin calcium
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, (2017/12/27)
The invention relates to a synthesis method of chiral isomer impurities of rosuvastatin calcium. The invention finds that meso compounds IV (3R, 5R) and (3R, 5S), which are obtained after a compound III is reduced by sodium borohydride, differ greatly in chemical properties, (3R, 5S) compounds, adopting hydroxyl cis-structures, on C-3 and C-5 can be hydrolyzed in a very low-temperature alkaline environment, while (3R, 5R) compounds, adopting hydroxyl trans-structures, on the C-3 and the C-5 can be hydrolyzed at a relatively high temperature and cannot be hydrolyzed at a low temperature, and by virtue of a peculiar phenomenon, two chiral isomers of the meso compound IV are separated to obtain a target compound. The synthesis method is short in route; chiral carbon is not required to be introduced from a side chain source; the synthesis method is simple in process and easy to operate; the purity and the yield of the obtained target product are high, the purity can reach 98.8%, the yield can reach 75%, and the purity and the yield are much higher than those in the prior art; a reference substance is provided for the (3R, 5S) chiral isomer impurities of the rosuvastatin calcium; the synthesis method is of a great significance in researching the quality of the rosuvastatin calcium.