辛伐他汀的合成工艺改进

Improvement of Synthesis of Simvastatin

本文对辛伐他汀合成路线进行了改进,以洛伐他汀为起始原料合成辛伐他汀。在羟基保护工序以二氯甲烷替代DMF为溶剂与叔丁基二甲基氯硅烷反应进行羟基保护,在甲基化工序以溴甲烷替代碘甲烷进行甲基化反应,甲基化产物经脱保护、脱丁胺、成铵盐、环化得到辛伐他汀。改进后的工艺不产生难处理的含DMF废水,对环境友好且成本更低廉。

In this paper, the synthetic route of simvastatin was improved. In the hydroxyl protection process, dichloromethane was used to replace DMF as solvent to react with tertbutyldimethylchlorosilane. In the methylation process, methyl bromide was used to replace methyl iodide. The improved process is more environmentally friendly and cheaper.