Steroidverbindung und Verfahren zu ihrer Herstellung

摘要

1,206,874. 7α-Methyl-6#,19-oxide-steroids. UPJOHN CO. 16 Feb., 1968 [15 March, 1967], No. 14554/70. Divided out of 1,206,872. Heading C2U. Novel steroids of the formula (wherein the 1,2- and 4,5-carbon atom linkages are single or double bonds, the 5#-hydrogen atom being absent in the #4-compounds, R11 is H or C 1-12 carboxylic acyl; R is H or C 1-12 alkyl; and X is H or Br; provided that when X is Br then ring A is saturated, and when X is H then ring A is saturated or has one double bond only) are prepared by the light catalysed reaction of I7α-R-6#-hydroxy-7α-methyl-testosterone 17-acylates with lead tetra-acetate to give the required #4-17#-acyloxy compounds or the iodine catalysed reaction of the corresponding ring A-saturated starting materials with lead tetra-acetate (with or without intermediate protection of the 3-keto group as an alkylene ketal) to give the required ring A-saturated- 17#-acyloxy compounds, followed, when required, by bromination of the last-named products to give the required 2-bromo-compounds with, when required, subsequent dehydrobromination of these to give the required #1-compounds. The 17-acylates thus-prepared may be hydrolysed to the free 17#-ols. The novel steroids are stated to possess anabolic, androgenic, progestational, anti-fertility, cholesterol-lowering and CNS-depressant activity, and they may be made up into pharmaceutical compositions with suitable carriers. Specifications 1,206,872 and 1,206,873 are referred to.