Improvements in or relating to steroids and the manufacture thereof

摘要

The invention comprises a steroid g -lactone selected from the formulae consisting of wherein R1 is or keto oxygen, in which Ac is the acyl group of a hydrocarbon carboxylic acid containing 1-12 carbon atoms, wherein R2 is or keto oxygen in which Ac is defined as above; wherein R3 is hydrogen or methyl; wherein R4 is an alkylene radical containing not more than eight carbon atoms, and the attaching oxygen to carbon bonds are separated by a chain of at least 2 and not more than 3 carbon atoms; and wherein X is chlorine, fluorine or methyl, and wherein the linkages of the carbon atoms in positions 1, 2 and 4, 5 of Formula I are single bonds, the combination of one double bond in positions 4, 5 and a single bond in position 1, 2 or the combination of 2 double bonds, with the proviso that if the compound of Formula I has no 4,5-double bond, the 5-carbon atom as a substituent selected from a -hydrogen or b -hydrogen, a steroid q -lactone 3-ester of the formula wherein R1 is wherein R2 is or keto oxygen, and wherein the linkage between carbon atoms 5 and 6 is a single or double bond, and a process for the production of a 16hydroxy - 17(20) - pregnen - 21 - oic acid q lactone which comprises treating a 16-hydroxytrans -17(20) - pregnen - 21 - oic acid with an organic sulphonyl halide of the formula ROSO2X in which R is alkyl, aryl, or aralkyl, containing up to and including 10 carbon atoms, and in which X is chlorine or bromine, or an acid anhydride of a hydrocarbon carboxylic acid containing 2-12 carbon atoms, to obtain a 16-hydroxy -17(20)-pregnen-21-oic acid q -lactone. Pharmaceutical compositions having cytotoxic, antibacterial, and tranquilizing activity comprise the above compounds and a pharmaceutical carrier.