Procédé de préparation de stéroïdes

1,271,984. 7-Hydroxylated steroids. E. R. SQUIBB & SONS Inc. 28 Feb., 1969 [15 March, 1968], No. 10895/69. Heading C2U. [Also in Division C5] The invention comprises compounds of formula wherein R is H or acyl; P and Q are each H, C 1-8 alkyl, C 1-8 haloalkyl, C 3-6 cycloalkyl, (C 3-6 cycloalkyl...

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Hauptverfasser: ANDREW DIASSI,PATRICK, ANTHONY PRINCIPE,PACIFICO
Format: Patent
Sprache:fre
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Zusammenfassung:1,271,984. 7-Hydroxylated steroids. E. R. SQUIBB & SONS Inc. 28 Feb., 1969 [15 March, 1968], No. 10895/69. Heading C2U. [Also in Division C5] The invention comprises compounds of formula wherein R is H or acyl; P and Q are each H, C 1-8 alkyl, C 1-8 haloalkyl, C 3-6 cycloalkyl, (C 3-6 cycloalkyl)-(C 1-8 alkyl), "aryl", "aryl"- (C 1-8 alkyl), monocyclic heterocyclyl or (monocyclic heterocyclyl)-(C 1-8 alkyl), provided that P and Q are not both H; or P and Q together with the intervening carbon atom are C 3-6 cycloalkylidene or monocyclic heterocyclic ylidene. "Aryl" signifies phenyl and substituted phenyl. Preparation of the above is from the corresponding 7 - unsubstituted - 21 - (free hydroxy) compounds by enzymatic hydroxylation with Thamnidium elegans, followed, when required, by 7, 21-diacylation. Basification of the inventive compounds (having R=acyl) results in #4,6-7-unsubstituted- 21-ols which may be re-esterified at the 21- position. The inventive compounds are said to possess progestational, adrenocortical and anti-inflammatory activities, and may be made up with carriers into pharmaceutical compositions for oral, parenteral and topical administration.