The invention belongs to the field of pharmaceutical
chemistry synthesis, and relates to a preparation method for a key intermediate 2alpha, 3alpha-
epoxy-16beta-(1-pyrrolidyl)-5alpha-
androstane-17 hydroxy of
rocuronium bromide of
steroid muscle relaxant, which includes the steps: leading inexpensive and available 5alpha-
androstane-2-
alkene-17
ketone and
isopropenyl acetate to undergo ester exchange to generate cresyl violet acetate, oxidizing the cresyl violet acetate by the meta-chloroperoxybenzoic acid to obtain an
epoxy compound, carrying out an open-loop
substitution reaction between the meta-chloroperoxybenzoic acid and
pyrrolidine under the alkaline condition, and reducing via
sodium borohydride so that the
rocuronium bromide key intermediate 2alpha, 3alpha-
epoxy-16beta-(1-pyrrolidyl)-5alpha-
androstane-17 hydroxy is prepared. An ester group with large steric hindrance is generated at the 17th position when the 5alpha-androstane-2-
alkene-17
ketone and the
isopropenyl acetate undergo ester exchange in the process to lead stereoscopic steric hindrance of a whole
steroid ring to be large, so that
attack on the lower portion of the
steroid ring can be performed when epoxidation is carried out, and further
stereoselectivity is high when an
epoxide is formed, and then a beta configuration can be directly formed when the
pyrrolidine is used for substitution. The synthesis method is good in
stereoselectivity.