摘要
以4-(4-氟苯基)-6-异丙基-2-(N-甲基-N-甲磺酰基氨基)嘧啶-5-甲醇为起始原料,经缩合、水解去保护、酯化、水解、成钙盐等反应,重新设计并优化了缩合工艺和纯化工艺,制得降血脂药瑞舒伐他汀钙,合成的目标化合物,总收率为34.3%,纯度达到99.5%以上。并通过质谱、核磁共振氢谱和碳谱对目标产物进行了结构表征。本工艺操作简单,成本较低,收率和纯度较高,适合工业化生产。
Starting with N-（5-（（diphenylphosphoryl）methyl）-4-（4-fluorophenyl）-6-isopropylpyrimidin-2-yl）-N-methylmethanesulfonamide（C28H29FN3O3PS）,rosuvastatin calcium was prepared through condensation,hydrolysis and deprotection,esterification,hydrolysis,salting.The process was redesigned and the optimum technological conditions were investigated.Thus,the total yield reached 34.3%,HPLC purity 99%.The structure was determined by MS,CNMR and HNMR.The process exhibits simple,cost-efficient,high purity and yield,easy to scale up.
出处
《广州化工》
CAS
2011年第8期54-55,共2页
GuangZhou Chemical Industry
基金
中山市健康产业专项资金
中山市科技型中小企业技术创新基金(基金编号:2007CX002)
