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PubMed1995

[Acetylation of spironolactone, canrenone and 2-methyl-canrenone].

Reaction of the title compounds with acetic anhydride and acetyl chloride yields the 3,5-dien-3-yl acetate 2, the isomeric 2,4,6- and 3,5,7-trien-3-yl acetates 3 and 4 as well as the 2,4,6,8(14)-tetraen-3-yl acetate 7. The 2 alpha-methyl-8,14-didehydro-canrenone (9) is obtained by hydrolysis of 7. Binding affinities of 7 and 9 to hormone receptors as well as serum proteins (SHBG, CBG) are investigated. The compounds are inactive.

Acetylation↗