文献类型：期刊文献

中文题名：抗组胺药非索非那定盐酸盐的合成

英文题名：Synthesis of fexofenadine hydrochloride as an anti-histamine drug

作者：吕彬华[1];杨雪艳[1];吴范宏[1]

机构：[1]华东理工大学化学与制药学院,上海200237

年份：2004

卷号：14

期号：2

起止页码：96

中文期刊名：中国药物化学杂志

外文期刊名：Chinese Journal of Medicinal Chemistry

收录：CSTPCD;;CSCD:【CSCD_E2011_2012】；

语种：中文

中文关键词：药物化学;工艺改进;化学合成;非索非那定盐酸盐;2-甲基-2-苯基丙酸

外文关键词：medicinal chemistry;process improvement;chemical synthesis;fexofenadine;α,α-dimethylphenylacetic acid

摘要：目的研究抗组胺药非索非那定盐酸盐 (fexofenadinehydrochloride)的合成。 方法以 2 甲基 2 苯基丙酸为起始原料 ,通过氯化、胺化、傅 克酰基化、缩合、还原、水解及成盐 7步反应 ,合成得到非索非那定盐酸盐 (1)。结果与结论以总产率为 38 1%合成得到非索非那定盐酸盐 ,其结构经核磁 (1H NMR)和质谱 (MS)确证。本法具有原料价廉易得、反应条件温和、操作简便等优点。适合于工业化生产。
Aim To improve the synthetic procedure of fexofenadine hydrochloride.Methods Starting from 2-methyl-2-phenyl-propionic acid,the target compound can be obtained through seven steps such as chlorination,amination,Friedel-Crafts acylation,condensation,reduction,hydrolysis and salt formation,etc..Results and Conclusion The total yield was 38.1%.The structure has been established by 1H-NMR and MS.The procedure developed has several advantages of cheap reagents,facile reaction conditions,convenient operation,and is suitable for industrial production.