Ⅰ晶型硫酸氢氯吡格雷的合成

Synthesis of clopidogrel bisulfate of crystal form Ⅰ

目的:合成Ⅰ晶型硫酸氢氯吡格雷。方法:对S构型的氯吡格雷游离碱用左旋樟脑磺酸成盐来拆分进行光学纯度的提高;在甲醇-甲基叔丁基醚系统中将Ⅱ晶型转化得到I晶型。结果与结论:获得高纯度硫酸氢氯吡格雷,工艺适合工业化生产。

Objective： To synthesize clopidogrel bisulfate of crystal form I . Methods： The optical purity of clopidogrel free alkali of S configuration was improved by salification reaction with L-camphorsulphonic acid; crystal form Ⅱ was converted to crystal form I in a solvent system consisting of methanol and methyl tert-butyl ether. Results and Conclusion ： Clopidogrel bisulfate of high purity is obtained and the process is industrially applicable.