| 摘要 |
<p>The invention comprises steroid 16b -hydroxy-21-carboxylic acid g -lactones represented by the following formulae <FORM:1031746/C2/1> <FORM:1031746/C2/2> <FORM:1031746/C2/3> <FORM:1031746/C2/4> <FORM:1031746/C2/5> <FORM:1031746/C2/6> <FORM:1031746/C2/7> <FORM:1031746/C2/8> <FORM:1031746/C2/9> <FORM:1031746/C2/100> <F wherein the 1,2-carbon atom linkage is a single or a double bond linkage, R is hydrogen or the acyl radical of a hydrocarbon carboxylic acid containing from 1-12 carbon atoms, inclusive, W is a methylene, b -hydroxymethylene, carbonyl, a -hydroxymethylene, or a -acyloxymethylene group, R2 being the acyl radical of a hydrocarbon carboxylic acid containing from 1-12 carbon atoms, inclusive, and provided that R2 is the same as R when R is an acyl radical, X is the group b -hydroxymethylene or carbonyl, Y is the methylene group, b -hydroxymethylene group or carbonyl group, Z is a hydrogen or fluorine atom, and X and Z and Y and Z can together constitute a 9(11)-double bond, the corresponding 16b -hydroxy-17a -iodo, bromo or chloro-pregna-21-oic acid lactones and a process for the production thereof which comprises (a) reacting a pregnane having at ring D the structure: <FORM:1031746/C2/122> wherein R1 is hydrogen or methyl, with iodine, bromine, or chlorine in an aqueous alkaline medium to obtain a 17a -haloactone steroid having at ring D the structure <FORM:1031746/C2/133> wherein V is iodine, bromine, or chlorine and (b) reacting the thus obtained 17a -halolactone with a dehydrohalogenating agent to obtain the desired 16a -hydroxy-21-carboxylic acid g -lactone steroid.ALSO:Pharmaceutical compositions having cardiotonic, anti-inflammatory, salt and water-regulating, pituitary inhibiting, anti-anabolic, muscle relaxant, antifertility, cytotoxic anti-viral and anti-microbial activities and also useful as ultraviolet screens and containing steroid 16b -hydroxy-21-carboxylic acid g -lactones of the pregnane series having in ring D the structure <FORM:1031746/A5-A6/1> wherein R1 is H or methyl, are administered orally, by injection, or topically with coacting antibiotics, or germicides.</p> |
