| 摘要 |
1,269,225. #<SP>9(11)</SP>-Steroids. E. R. SQUIBB & SONS Inc. 28 March, 1969 [2 April, 1968], No. 16336/69. Heading C2U. Compounds of Formula VII (wherein Y is a single or double bond, Ac is C 1-12 acyl, P is H, C 1-8 alkyl, C 1-8 haloalkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl - C 1-8 alkyl, " aryl " or " aryl "-C 1-8 alkyl, and Q is C 1-8 alkyl, C 1-8 haloalkyl, " aryl " or " aryl "-C 1-8 alkyl (" aryl " signifying optionally substituted phenyl), or P, Q and the intervening carbon atom together form C 3-6 cycloalkylidene) are prepared from compounds of Formula I by the successive steps of (i) microbial 11α- hydroxylation, (ii) acylation of the 21-hydroxy group, (iii) mesylation of 11α-hydroxy group, and (iv) elumination of MeSO 3 H to introduce #<SP>9(11)</SP>-unsaturation. Compounds VII are interconvertible by 1,2-dehydrogenation (e.g. with DDQ) of the 1,2-saturated compounds. Acetals and ketals of triancinolone and 1,2. dihydro derivatives thereof are obtainable from compounds VII by effecting the conversions: #<SP>9(11)</SP> # 9α - bromo - 11# - hydroxy # 9#,11# - epoxy # 9α - fluoro - 11# - hydroxy, followed by hydrolysis of the 21-acyloxy group. Compounds of Formula I are prepared by acetalization of 16α - hydroxycortexolone followed, when required, by 1,2-dehydrogenation (which may be effected after 21-acylation). |
