| 摘要 |
Novel 10 beta -alkynyl-steroids of the formula <IMAGE> I wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R6 and R7 taken together with the carbon atoms to which they are attached form cyclopropyl or R6 is hydrogen and R7 is R1, R1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of <IMAGE> <IMAGE> Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is <IMAGE> or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of -CH2-CH2-CH2-OH, hydrogen, R4, and -CH2-CH2-COOM, M is selected from the group consisting of hydrogen, -NH4 and alkali metal and R4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R6 and R7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R6 and R7 may be in the alpha or beta position with the proviso that R is not hydrogen when R6 and R7 are hydrogen, R2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.
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