阿伐斯汀的合成研究  

Synthesis of acrivastine

作　　者：石静波[1] 李荣[1] 彭磊[1] 陆维丽[1] 

机构地区：[1]安徽医科大学药学院,合肥230032

出　　处：《中国新药杂志》2009年第22期2176-2178,共3页Chinese Journal of New Drugs

基　　金：安徽省高校青年教师科研资助计划项目(2006JQ1105)

摘　　要：目的:合成抗组胺药物阿伐斯汀。方法:以2,6-二溴吡啶为起始原料,经酰化反应,HECK反应得到(E)-3-[6-[(4-甲苯基)羰基]-2-吡啶基]丙烯酸乙酯,再经Wittig反应得到(E)-6-[(E/Z)-3-(1-吡咯烷基)-1-(4-甲基苯基)丙烯基]-2-吡啶丙烯酸乙酯,经酸转化,水解,重结晶得阿伐斯汀。结果与结论:阿伐斯汀总收率17%,该法缩短了反应时间,反应条件温和,有较好的工业应用前景。Objective：To synthesize the antihistamine drug acrivastine.Methods：Started from 2,6-dibromopyridine,acrivastine was synthesized by acylation reaction,HECK reaction to obtain（E）-3-[6-（4-Methyl-benzoyl）-pyridin-2-yl]-acrylic acid ethyl ester,which was reacted by Wittig condensation affords a cis：trans mixture of（E）-6-[3-（1-Pyrrolidinyl）-1-p-tolyl-propenyl]-2-pyridin-eacrylic acid ethyl ester;then treated with acid,hydrolization and recrystallization.Results and Conclusion：The total yield of acrivastine wasover 17%. The new process has the advantages, including short reaction period, mild reaction condition, with a good prospect for industrial application.

关 键 词：阿伐斯汀 组胺H1拮抗剂 合成 

分 类 号：R976[医药卫生—药品]