9-ALPHA-HYDROXY STEROIDS,PROCESS FOR THEIR PREPARATION,PROCESS FOR THE PREPARATION OF THE CORRESPONDING 9(11)-DEHYDRO DERIVATIVES AND PHARMACEUTICAL PREPARATIONS CONTAINING SAID STEROIDS

摘要

9-Alpha-hydroxy- steroids (I) contg. a D-ring of formula (A) are new; R2 = ethynyl (provided R5 is not acetoxy if R4 = H), haloethynyl, opt. protected OH, cyano, 1'-Ra-ethenyl; or 1',1'-trimethylene dithio-ethyl; Ra = 1-6C alkoxy or alkylthio, aryloxy or arylthio; R3 = H; R4 = H, OH, alpha or beta-Me or R3and R4 are together = CH2, or R2 and R3 are together a double bond; R5 = CN, COCHR1R1', CONH2, OH, opt. halo-substd. ethynyl; sulphonate, sulphite, trialkylsilyloxy, formyloxy, opt. halo-substd. 1-6C acyloxy, C(=NR80)Me, C(NHR82)=CH2 or C(=NR80)CH2X; X = halo; R80 = H, COR81 or trialkylsilyl; R81 = H, 1-6C alkyl or phenyl (opt. substd. by 0-2 chloro, Me or NO2); R82 = COR81, trialkylsilyl or R2 and R5 are together carbonyl (provided R4 is not H); R1 = halo or opt. substd. benzoyloxy or (provided R4 is not H)OH, opt. halogenated 1-6C carboxylic acyloxy or H; R'1 = H, Cl, Br or I.