| 摘要 |
1288414 Steroid 21-cyclobutane esters FARBWERKE HOECHST AG 22 Sept 1969 [20 Sept 1968] 46559/69 Heading C2U The invention comprises compounds of formula represents (i) a Y . . . C 9 -C 11 =X group where Y is H or F and X is H 2 , OXO, H(#-OH), H(α-OH), H(#-Cl) or H(#-F), or group; R 1 represents H 2 , H(α-Me), H(#-Me), H(α-F), H(#-F), CH 2 , CHF or CF 2 ; R 2 represents H or OH; R 3 represents a direct bond or a C 1-5 divalent aliphatic hydrocarbon group; and R 4 represents a cyclobutyl group which is substituted by at least one fluorine atom and which may be further substituted by one or more methyl groups and/or chlorine atoms. Preparation of the above compounds is from the corresponding steroid 21-ols by reaction with a compound of formula Cl-CO-R 3 -R 4 . Product interconversions specified are 1,2- and/ or 6,7-dehydrogenation; 6-, 9-, 11- and/or 16- fluorination; further fluorination of the cyclobutane ring; and reduction of 11-oxo to 11- hydroxy. The inventive compounds are stated to possess anti-inflammatory activity and may be made up with carriers into pharmaceutical and veterinary compositions for topical administration.
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