| 摘要 |
1,164,585. α - (3 - Benzoylphenyl) alkanoic acid derivatives. RHONE-POULENC S.A. 26 Jan., 1968 [27 Jan., 1967; 15 Dec., 1967], No. 4326/68. Heading C2C. Novel compounds of formula and salts thereof wherein R is H or C 1-4 alkyl, R 1 is H or C 1-4 alkylthio and R 2 is H, OH or methoxy including the DL, L and D forms when R is alkyl, are prepared by one of the following methods; (a) by hydrolysing and decarboxylating a compound of general Formula II wherein R 3 and R 4 are C 1-4 alkyl; (b) by oxidation of a compound of Formula VII or (c) by hydrolysis of a compound of general Formula IV and optionally followed in all cases by salt formation. Cyanoesters of Formula II above are prepared by alkylation of a compound of formula which is itself prepared by reaction of a compound IV above with an alkyl carbonate of formula R 4 O.CO.OR 4 . Benzoylphenylacetonitriles of Formula IV above are prepared by action of an alkalimetal cyanide on a 3-halomethylbenzophenone of formula which is itself prepared by halogenation of the corresponding methyl compound. Benzylphenylalkanoic acids of Formula VII above are prepared by desulphurization of a thioxanthone of formula which may be obtained in optically active forms by resolution via the α-phenylethylamine salt after formation of the racemate by cyclization of a diphenyl sulphide of formula which is itself prepared from 2-iodobenzoic acid and a thiophenol of formula prepared by the action of potassium ethylxanthate on the diazonium salt of an amine of formula Pharmaceutical compositions in conventional forms for oral, rectal, topical or parenteral administration and having anti-inflammatory activity comprise an above novel compound or salt and one or more carriers or diluents therefor. |
