119302-24-8Relevant articles and documents
Preparation method of rocuronium bromide intermediate and rocuronium bromide
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Paragraph 0014; 0041-0042; 0044-0045; 0047-0048; 0050-0051, (2020/03/06)
The invention discloses a preparation method of a rocuronium bromide intermediate and rocuronium bromide. According to the method, (2beta,3alpha,5alpha,16beta,17beta)-2-(4-morpholinyl)-16-(1-pyrrolidinyl)androstane-3,17-diol is used as an initial raw material, and is subjected to selective acetylation with glacial acetic acid under the action of a condensing agent to obtain (2beta,3alpha,5alpha,16beta,17beta)-2-(4-morpholinyl)-16-(1-pyrrolidinyl)androstane-3,17-diol-17-acetate, and then (2beta,3alpha,5alpha,16beta,17beta)-2-(4-morpholinyl)-16-(1-pyrrolidinyl)androstane-3,17-diol-17-acetate issubjected to salt formation with 3-bromopropene in a protic solvent under the action of a basic catalyst to obtain rocuronium bromide. The preparation method adopted in the invention is mild in reaction conditions, simple in post-treatment, and suitable for large-scale industrial application.
A new and efficient method for the synthesis of rocuronium bromide
Wu, Xue-Ying,Wang, Yao-Ling,Hai, Li,Gong, Ping,Wu, Yong
, p. 487 - 492 (2017/01/28)
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.
NOVEL METHOD FOR SYNTHESIS OF NEUROMUSCULAR BLOCKING AGENTS
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Page/Page column 12, (2016/03/13)
The invention discloses a novel method for preparing neuromuscular blocking agents using aryl esters as a reagent of di-acylation as well as highly regioselective mono-acylation of androstane-diols.