Study On The Process Of A New Generation Of Progesterone Drospirenone

Drospirenone is a highly efficient,low toxicity and good safety of a new generation of hormone,firstly developed by the German Schering company.Many methods for the preparation of drospirenone were reported.Taking the commercially available 3?,5-dihydroxy-6?,7?;15?,16?-dimethylene-5?-androstan-17-one as the starting material,the synthesis of drospirenone was fulfilled through multi-steps.Firstly,the catalogs and their action mechanism of progesterone drugs were reviewed in the first chapter.Secondly,a novel method for the synthesis of drospirenone was designed and investigated,which involved addition of carbonyl group with propargyl anion,hydrogenation,oxidation and dehydroxylation.Among them,the various parameters of each steps were studied in detail,such as temperature,solvents,ratio of reagents.The optimal conditions are obtained.Furthermore,the structure of the final product drospirenone was confirmed by FT-IR,HNMR and MS spectrometer.This synthetic route has some advantages such as short steps,mild conditions,low cost,high yield.The process and the operation equipment are simplified.It has good values for the industrilaztion of drospirenone.