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A new and efficient method for the synthesis of rocuronium bromide
Alternative TitleA new and efficient method for the synthesis of rocuronium bromide
Wu XueYing1; Wang YaoLing2; Hai Li2; Gong Ping1; Wu Yong2
2017
Source PublicationCHINESE CHEMICAL LETTERS
ISSN1001-8417
Volume28Issue:2Pages:487-492
AbstractRocuronium 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 2 beta-(4morpholiny1)-16 beta-(1-pyrrolidiny1)-5 alpha-androstan-3 alpha,17 beta-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. (C) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
Other AbstractRocuronium 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.
KeywordULIPRISTAL ACETATE DERIVATIVES RECEPTORS THIAZOLE PYRAN HL-60 Rocuronium bromide 2 alpha,3 alpha-Epoxy steroid derivative NMBAs Fe-mediated New route
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation]
CSCD IDCSCD:5934409
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/153905
Collection中国科学院金属研究所
Affiliation1.中国科学院金属研究所
2.四川大学
Recommended Citation
GB/T 7714
Wu XueYing,Wang YaoLing,Hai Li,et al. A new and efficient method for the synthesis of rocuronium bromide[J]. CHINESE CHEMICAL LETTERS,2017,28(2):487-492.
APA Wu XueYing,Wang YaoLing,Hai Li,Gong Ping,&Wu Yong.(2017).A new and efficient method for the synthesis of rocuronium bromide.CHINESE CHEMICAL LETTERS,28(2),487-492.
MLA Wu XueYing,et al."A new and efficient method for the synthesis of rocuronium bromide".CHINESE CHEMICAL LETTERS 28.2(2017):487-492.
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