A new and efficient method for the synthesis of rocuronium bromide

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• 作者：Xue-Ying Wu^a ; Yao-Ling Wang^b ; Li Hai^b ; Ping Gong^a ; ^{gongpinggp@126.com} ; Yong Wu^b ; ^{wyong@scu.edu.cn}
• 关键词：Rocuronium bromide ; 2α ; 3α-Epoxy steroid derivative ; NMBAs ; Fe-mediated ; New route
• 刊名：Chinese Chemical Letters
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：28
• 期：2
• 页码：487-492
• 全文大小：720 K
• 卷排序：28

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.