| 摘要 |
1,206,915. Derivatives of indole and 4,5,6,7- tetrahydroindole. STERLING DRUG Inc. 12 Feb., 1969 [20 Feb., 1968], No. 7719/69. Heading C2C. The invention comprises compounds of formulae wherein R 1 is H or C 1-6 alkyl; R 2 is H, C 1-6 alkyl, CO 2 (R 1 ) or CH 2 OH; R 3 is Ph, Ph-C 1-6 -alkyl, PhCOCH : CH or Z-CO where Z is Ph, biphenylyl, thienyl, furyl, pyridyl, isoxazolyl, thiazolyl, isothiazolyl, cycloalkyl, adamantyl, Ph-C 1-5 -alkyl or Ph-C 2-5 -alkenyl (each Ph being optionally substituted by the radicals indicated for R 4 ; R 4 is H, 1 or 2 methylenedioxy or ethylenedioxy groups, or up to 4 halogen, C 1-6 alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl, NO 2 , NH 2 , C 1-6 -alkanoylamino, di-(C 1-6 -alkyl)amino, CF 3 , C 1-6 alkanoyloxy or OH (excluding C 1-6 alkoxy as a single substituent); Y is C 1-6 alkylene; and basic salts of those compounds where R 1 is H. The indole derivatives are prepared by reacting the corresponding 1-unsubstituted indoles (in practice as the 1-Na compound made in situ with NaH) with X-Y-CO 2 (R<SP>1</SP>) (X = halogen); the acids (R 1 = H) are also prepared by alkaline hydrolysis of the esters (R 1 = C 1-6 alkyl). The tetrahydroindole derivatives are prepared (a) where R 3 is acyl, by reacting the corresponding 3-unsubstituted tetrahydroindoles with R 3 X in presence of a Lewis acid, or (b) where R 3 is Ph, byreacting in an acidic medium, an optionally R 4 -substituted 2-(R 2 COCHPh)-cyclohexanone with NH 2 -Y-CO 2 (R 1 ); in either case, acids so formed may be esterified, and esters may hydrolysed. Therapeutic compositions in the form of suspensions, emulsions, tablets or capsules, comprise compounds of the above formulµ which have anti-inflammatory activity. |
