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A new and efficient method for the synthesis of rocuronium bromide

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Wu Xueying 1   Wang Yaoling 2   Hai Li 2   Gong Ping 1 *   Wu Yong 2 *  
文摘 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.
来源 Chinese Chemical Letters ,2017,28(2):487-492 【核心库】
DOI 10.1016/j.cclet.2016.10.026
关键词 Rocuronium bromide ; 2α,3α-Epoxy steroid derivative ; NMBAs ; Fe-mediated ; New route
地址

1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang, 110016  

2. West China School of Pharmacy, Sichuan University, Key Laboratory of Drug Targeting and Drug Delivery Systems of Ministry of Education, Chengdu, 610041

语种 英文
文献类型 研究性论文
ISSN 1001-8417
学科 化学工业
基金 support from the National Natural Science Foundation of China
文献收藏号 CSCD:5934409

参考文献 共 36 共2页

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引证文献 1 篇

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