A new and efficient method for the synthesis of rocuronium bromide  

作　　者：Xue-Ying Wu Yao-Ling Wang Li Hai Ping Gong Yong Wu 

机构地区：[1]Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University [2]Key Laboratory of Drug Targeting and Drug Delivery Systems of Ministry of Education, West China School of Pharmacy, Sichuan University

出　　处：《Chinese Chemical Letters》2017年第2期487-492,共6页中国化学快报（英文版）

基　　金：the National Natural Science Foundation of China (No. 81373259 & No. 81573286)

摘　　要：Rocuronium bromide has been used as an aminosteroid non-depolarizing neuromuscular blocker and muscle relaxant.In this work,a new and efficient route for preparing a key intermediate 2β-（4-morpholinyl）-16β-（1-pyrrolidinyl）-5α-androstan-3α,17β-diol（6） was developed through a ring-opening of epoxide followed by introducing and pyrrolidine.Compound 6 can easily provide rocuronium bromide and the overall yield of compound 6 in 5 steps increased to 57.8%,which was higher than currently reported methods.Extraordinarily,this method would avoid the generation of disubstituted impurities E and F which are difficult to remove.Rocuronium bromide has been used as an aminosteroid non-depolarizing neuromuscular blocker and muscle relaxant.In this work,a new and efficient route for preparing a key intermediate 2β-（4-morpholinyl）-16β-（1-pyrrolidinyl）-5α-androstan-3α,17β-diol（6） was developed through a ring-opening of epoxide followed by introducing and pyrrolidine.Compound 6 can easily provide rocuronium bromide and the overall yield of compound 6 in 5 steps increased to 57.8%,which was higher than currently reported methods.Extraordinarily,this method would avoid the generation of disubstituted impurities E and F which are difficult to remove.

关 键 词：Rocuronium bromide 2α 3α-Epoxy steroid derivative NMBAs Fe-mediated New route 

分 类 号：TQ463[化学工程—制药化工]