合成盐酸氨溴索的新方法  

New Method for The Synthesis of Ambroxol Hydrochloride

作　　者：李聪豪 潘鹏 郭红云[1] LI Cong-hao;PAN Peng;GUO Hong-yun(College of Chemical Engineering,Zhejiang University of Technology,Hangzhou 310014,China)

机构地区：[1]浙江工业大学化学工程学院

出　　处：《合成化学》2019年第10期820-822,855,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以邻氨基苯甲酸甲酯(1)为起始原料,与溴素发生溴化反应制得2-氨基-3,5-二溴苯甲酸甲酯(2);2经红铝试剂还原制得2-氨基-3,5-二溴苯甲醛(3);3经还原胺化制得氨溴索(4);4盐酸化得到盐酸氨溴索(5),总收率60.8%,其结构经1HNMR确证。Methyl 2-amino-3,5-dibromobenzoate( 2 ) was synthesized from methyl anthranilate( 1 ) via bromination reaction,followed by reduction to give 2-amino-3,5-dibromobenzaldehyde( 3 ). Ambroxol( 4 ) was prepared by reductive amination from 3 . Finally,ambroxol hydrochloride( 5 ) with an overall yield of 60.8% was synthesized through hydrochloric acid reaction. The structure was confirmed by ^1 H NMR.

关 键 词：邻氨基苯甲酸甲酯 红铝 还原胺化 盐酸氨溴索 药物合成 

分 类 号：O625.42[理学—有机化学] R914.5[理学—化学]