东南大学学报（英文版）2008，Vol.24Issue(2)：247-249,3.
一种大规模合成N-(4-羟苯基)维甲酰胺的新方法
Novel process for large scale synthesis of N-(4-hydroxyphenyl) retinamide
吴晓晴 1余佳 1吉民1
作者信息
- 1. 东南大学化学化工学院,南京,210009
- 折叠
摘要
Abstract
A method to synthesize anticancer drug N-( 4-hydroxyphenyl) retinamide (4-HPR)on a large scale is described.It consists of the preferred steps of reacting all-trans retinoic acidwith thionyl chloride to form retinoyl chloride and then reactingwith triethylamine to generate retinoyl ammonium salt which inturn is reacted with p-aminophenol to eventually produce 4-HPR.This process can overcome many scale-up challenges that exist inthe methods reported in the literature and provide an easy, mildand high yield route for large scale synthesis of 4-HPR.Moreover, the effects of the molar ratios of the reagents on theyield are examined. The best molar ratios are a 2.0 molarequivalence of thionyl chloride and a 3.0 molar equivalence of p-aminophenol to retinoic acid, and the total yield is 80. 7%.关键词
4-HPR/大规模/合成/抗肿瘤Key words
4-HPR/ large scale/ synthesis/ anticancer分类
化学化工引用本文复制引用
吴晓晴,余佳,吉民..一种大规模合成N-(4-羟苯基)维甲酰胺的新方法[J].东南大学学报（英文版）,2008,24(2):247-249,3.
