A new and efficient method for the synthesis of rocuronium bromide
查看参考文献36篇
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文摘
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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. |
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来源
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Chinese Chemical Letters
,2017,28(2):487-492 【核心库】
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DOI
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10.1016/j.cclet.2016.10.026
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关键词
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Rocuronium bromide
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2α,3α-Epoxy steroid derivative
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NMBAs
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Fe-mediated
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New route
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地址
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1.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang, 110016
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West China School of Pharmacy, Sichuan University, Key Laboratory of Drug Targeting and Drug Delivery Systems of Ministry of Education, Chengdu, 610041
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语种
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英文 |
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文献类型
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研究性论文 |
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ISSN
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1001-8417 |
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学科
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化学工业 |
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基金
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support from the National Natural Science Foundation of China
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文献收藏号
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CSCD:5934409
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参考文献 共
36
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