奥美沙坦酯杂质A和C的合成.pdfVIP

Pharmacy Information 药物资讯, 2016, 5(2), 9-13 Published Online May 2016 in Hans. /journal/pi /10.12677/pi.2016.52002 Syntheses of Impurity A and C of Olmesartan Medoxomil Weisi Li, Guoping Chen, Xin Fan, Jingyu Tang Jiangsu Zhongbang Pharmaceutical Co., Ltd., Nanjing Jiangsu th th th Received: Mar. 30 , 2016; accepted: Apr. 26 , 2016; published: Apr. 29 , 2016 Copyright © 2016 by authors and Hans Publishers Inc. This work is licensed under the Creative Commons Attribution International License (CC BY). /licenses/by/4.0/ Abstract 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 ob- tained by acidic-removal of Trt protecting group of starting material 1 with subsequent recrystal- lization 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. Keywords Olmesartan Medoxomil, Impurity A and C, Syntheses 奥美沙坦酯杂质A和C的合成 李维思，陈国萍，范 鑫，唐景玉 江苏中邦制药有限公司，江苏 南京 收稿日期：2016年3月30 日；录用日期：2016年4月26 日；发布日期：2016年4月29 日 文章引用: 李维思, 陈国萍, 范鑫, 唐景玉. 奥美沙坦酯杂质A 和C 的合成[J]. 药物资讯, 2016, 5(2): 9-13. /10.12677/pi.2016.52002 李维思 等 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