7-ALPHA-METHYL-ESTROGENS, PROCESS FOR THEIR PREPARATION AND THEIR USE IN FURTHER PROCESSING

摘要

For the Contracting States : BE, CH, DE, FR, GB, IT, LU, NL, SE 1.) 7alpha-methyl oestrogens of the general formula I see diagramm : EP0007516,P7,F1 in which R1 and R2 denote lower alkyl groups, X denotes a free or functionally protected hydroxymethylene group and Z denotes a hydrogen atom or an OR1 group. For the Contracting State : AT 1.) Process for the manufacture of compounds of the general formula I, see diagramm : EP0007516,P8,F1 in which R1 and R2 denote lower alkyl groups, X denotes a free or functionally protected hydroxymethylene group and Z denotes a hydrogen atom or an OR1 group, characterized in that, in a manner known per se, a) a compound of the general formula II see diagramm : EP0007516,P8,F2 in which R1 and Z have the meanings given above and R3 denotes a lower alkyl group or an optionally substituted aryl group, is reacted, in the presence of a deprotonating agent, with a compound of the general formula III see diagramm : EP0007516,P8,F3 in which X and R2 have the meanings given above, a compound of the general formula IV being obtained see diagramm : EP0007516,P8,F4 in which R1 , R2 , Z and X have the meanings given above ; b) the compound of the general formula IV is hydrogenated with a noble metal catalyst to form a compound of the general formula V see diagramm : EP0007516,P8,F5 in which R1 , R2 , Z and X have the meanings given above and c) the hydrogenation product of the general formula V, optionally after the addition of an oxidising agent, is subjected to equilibration and cyclisation and optionally protecting groups are split off.