Preparation of trialkylsilyloxy steroids having - oestrogenic, gestagenic and anabolic activity

摘要

Preparation of trialkylsilyloxy steroids having oestrogenic, gestagenic and anabolic activity. N3A. by reacting steroid alcohols with primary-, secondary, tertiary- and phenol hydroxy groups of general formula (I) (where R1 = O, ORY, OR5; OR5; OR7; R2 = H, OR5 or halogen; R3 is H2, = O, R5=H; R6 = H or lower alkyl (unless unsatd. bond is present); R7= Acyl (max C5), benzoyl, alkyl (max C5) or cyclopentyl; R8 = alkene or alkyne; R9 = H or halogen; R10 = H or Or5) with a trialkylchlorosilane and/or a hexaalkyldisilazane to give trialkylsilyloxy steroids of general formula (I) where R5 = trialkylsilyl or, in polyhydroxy steroids, trialkylsilyl and H. Excepted are compounds (Ie containing =O or H2 at posn. -3, together with a C=C- bond at posn 4 or 1- and 4, as well as H or satd. alkyl at posn. 17-alpha. Reaction is pref. carried out in a dipolar, aprotic solvent. (I) have oestrogenic-, gastagenic- and anabolic activity. They may also be used in the synthesis and purification of other medicaments.