SYNTHESIS OF 5-PREGNEN-3β, 17α-DIOL-20-ONE-3-ACET ATE-17α-CARBOX YLIC ACID ESTERS, AND STUDIES ON THEIR STRUCTURE-ACTIVITY RELATIONSHIPS
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Abstract
The syntheses of 17α-carboxylic acid esters of 5-pregnen-3β, 17α-diol-20-one-3 -acetate Ⅲ, Ⅳ (not reported previously) and Ⅴ are described. Animal tests (inflammatory granuloma pouch) gave the following results: the propanoic acid ester Ⅳ showed significant anti-inflammatory action, nearly equivalent to that of Antiflamisonum. The caproic acid ester Ⅴ has been found to Be somewhat more active than Antiflamisonum. D-Homo products obtained from the action of acidic aluminum oxide or alkali on 5-pregnen-3β, 17α-diol-20-one 3-acetate (Ⅱ) are studied.
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