标题:
奥美沙坦酯杂质A和C的合成Syntheses of Impurity A and C of Olmesartan Medoxomil
作者:
李维思, 陈国萍, 范鑫, 唐景玉
关键字:
奥美沙坦酯, 杂质A和C, 合成Olmesartan Medoxomil, Impurity A and C, Syntheses
期刊名称:
《Pharmacy Information》, Vol.5 No.2, 2016-04-29
摘要:
目的：优化和改进奥美沙坦酯杂质A和C的合成反应条件，提供了一条简单实用的合成奥美沙坦酯杂质A和C杂质对照品的路线。方法：杂质A由原料1通过一步酸解脱除三苯甲基保护基，然后用丙酮重结晶得到，而杂质C则通过原料2经叔醇官能团脱水成双键和酸解脱除三苯甲基保护基两步反应，最后通过柱层析得到。结果：优化了反应条件，重现性好，纯度大于95%符合杂质对照品要求。结论：本方法反应方法操作简单实用，重现性好。
Objective: A synthetic method towards impurity A and C of olmesartan medoxomil has been pro-vided through optimizing literature reaction conditions. Methods: Impurity A was directly obtained by acidic-removal of Trt protecting group of starting material 1 with subsequent recrystallization from acetone, whereas impurity C was afforded through dehydration of tertiary alcohol group of starting material 2 followed by acidic-removal of Trt protecting group. Results: Through optimization of literature reaction condition, impurity A and C with chemical purity greater than 95% can be readily obtained. Conclusion: The current method towards impurity A and C is simple and practical with good reproductivity.