[EN] PROCESS FOR THE PREPARATION OF ESTRADIOL AND ITS DERIVATIVES<br/>[FR] PROCÉDÉ DE PRÉPARATION D'OESTRADIOL ET DE SES DÉRIVÉS
申请人:RELIANCE LIFE SCIENCES PVT LTD
公开号:WO2012020417A1
公开(公告)日:2012-02-16
The present invention provides a process for the preparation of a compound of formula I wherein R1 represents a hydrogen atom, halogen atom, cyano group, hydroxyl group, straight or branched C1-C10 alkyl group, straight or branched C2-C10 alkenyl group or C6- C10 aryl group; or a -OR2, -O(CO)R2, or -R2-OH group, wherein R2 is a straight or branched Ci-C6 alkyl group or a straight or branched C2-C6 alkenyl group, which process comprises treating a compound of formula II wherein R1 is as defined above, with a compound of formula III M(BH4) III wherein M is a monovalent metal ion, in a solvent at a temperature of from -10 to 10°C.
本发明提供了一种制备式I化合物的方法,其中R1代表氢原子、卤素原子、氰基、羟基、直链或支链的C1-C10烷基、直链或支链的C2-C10烯基或C6-C10芳基;或者是一个-OR2、-O(CO)R2或-R2-OH基团,其中R2是直链或支链的Ci-C6烷基或直链或支链的C2-C6烯基,该方法包括将式II化合物(其中R1如上定义)与式III M(BH4) III化合物在溶剂中在-10至10°C的温度下处理。