中国药业2016，Vol.25Issue(2)：38-39,40,3.
普芦卡必利关键中间体4－氨基－5－氯－2，3－二氢－7－苯并呋喃苯甲酸的合成工艺研究
Synthesis of 4-Amino-5-Chloro-2,3-Dihydrobenzofuran-7-Carboxylic Acid, a Prucalopride′s Synthetic Intermediate
石权达 1闫冬 1高静 1姚宏涛1
作者信息
- 1. 辽宁亿灵科创生物医药科技有限公司，辽宁 本溪 117004
- 折叠
摘要
Abstract
Objective To study the synthetic process of 4-Amino-5-chloro-2,3-dihydrobenzofuran-7-carboxylic acid,the key intermediate for the preparation of prucalopride. Methods The target compound was prepared through demethylation,bromination,con-densation,cyclization and hydrolysis reaction with 2-methoxy-4-acetylamino-5-chloro methyl benzoate as starting material. Results The target compound was obtained through a 5-step procedure in an overall yield of 63%. The structure of target compound was con-firmed by 1HNMR and MS. Conclusion The easy availability of the reactants,facile reaction conditions and convenient operation pro-cedures make the process a promising prospect for application in large-scale manufacture.关键词
普芦卡必利/4-氨基-5-氯-2,3-二氢-7-苯并呋喃苯甲酸/合成Key words
prucalopride/4-Amino-5-chloro-2,3-dihydrobenzofuran-7-carboxylic acid/synthesis分类
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石权达,闫冬,高静,姚宏涛..普芦卡必利关键中间体4－氨基－5－氯－2，3－二氢－7－苯并呋喃苯甲酸的合成工艺研究[J].中国药业,2016,25(2):38-39,40,3.
