- Synthesis method of 16beta-tetrahydropyrrolyl androstan-2alpha-epoxy-17-one
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The invention relates to the technical field of medicines and chemical industry, discloses a preparation method of an important intermediate of rocuronium bromide, namely 16beta-tetrahydropyrrolyl androstan-2alpha-epoxy-17-one. The preparation method comprises the following steps: (1), in a ball milling tank, adding 17-acetoxy androstan-2alpha,16alpha-bisepoxide, pyrrolidine and silica gel, and reacting at a certain mechanical grinding frequency; and (2), post-treating a reaction mixture, and recrystallizing to obtain the 16beta-tetrahydropyrrolyl androstan-2alpha-epoxy-17-one. The preparationmethod has the advantages of high reaction yield, short time, high selectivity, simple and convenient operation, less pollution and the like, and is an environment-friendly chemical synthesis methodwith relatively good popularization and application prospects.
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Paragraph 0011; 0029-0053
(2019/01/14)
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- Processes for the synthesis of rocuronium bromide
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The invention encompasses processes for synthesizing 1-[17β-acetyloxy-3α-hydroxy-2β-(4-morpholinyl)-5α-androstan-16β-yl]-1-(2-propenyl)pyrrolidinium bromide (rocuronium bromide) and intermediates thereof.
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Page/Page column 11; 18
(2008/06/13)
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- Androstane derivatives substituted by a quaternary ammonium group in 16-position, pharmaceutical compositions containing them and process for preparing same
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There is disclosed novel, therapeutically active androstane derivatives having neuromuscular blocking effect, which are substituted by a quaternary ammonium group in 16-position; pharmaceutically composition containing them; process for producing them; and novel intermediates for the production.
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- Androstane derivatives substituted by a quaternary ammonium group in 16-position, pharmaceutical compositions containing them and process for preparing same
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There is disclosed novel, therapeutically active androstane derivatives having neuromuscular blocking effect, which are substituted by a quaternary ammonium group in 16-position; pharmaceutically composition containing them; process for producing them; and novel intermediates for the production.
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