Process for the preparation of pregn-4-ene-3,20-dione derivatives and 17-alpha-ethynyl-17-beta-trifluoroacetoxy-gon-4-ene-3-one derivatives, and pharmaceutical compositions containing the latter compounds

摘要

1. A process for preparing pregn-4-ene-3,20-dione derivatives having the general formula (I) see diagramm : EP0063368,P10,F1 wherein R1 represents a methyl or ethyl radical, R2 means hydrogen or a methyl radical, X represents a formyl or acetyl radical or hydrogen and the dotted lines (----) means further chemical bonds optionally present by reacting 17 beta-esters of 17 alpha-ethinyl-17 beta-hydroxy-gonane derivatives with formic acid or acetic acid in the presence of mercury salts as catalysts in dipolar aprotic or basic solvents, characterized in that one reacts as 17 beta-esters of 17 alpha-ethinyl-17 beta-hydroxygonane derivatives 17 alpha-ethinyl-17 beta-trifluoroacetoxygon-4-ene-3-one derivatives having the general (II) see diagramm : EP0063368,P10,F2 wherein R1 and R2 as well as the dotted lines are as above defined, in the presence of catalytic amounts of 1 or more dissociating mercury salt(s) in 1 or more dipolar aprotic or basic solvent(s) with formic acid or acetic acid and in a manner known per se optionally from the obtained pregn-4-ene-3,20-dione derivatives having the general formula I in which X represents a formyl or acetyl radical one splits off this.