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-pyr...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.展开更多
基金the National Natural Science Foundation of China (No. 81373259 & No. 81573286)
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.
