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[1] 陈国萍[1] 范鑫[1] 唐景玉 

机构地区：[1]江苏中邦制药有限公司,江苏南京

出　　处：《药物资讯》2016年第2期9-13,共5页Pharmacy Information

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.

关 键 词：奥美沙坦酯 杂质A和C 合成 

分 类 号：R9[医药卫生—药学]