Antiinflammatory, analgesic anilino-tropone derivs. - have few side effects on the gastric membrane

摘要

New anilinotropone derivs. are of formual (I) (where R is H or Me). (I) are prepd. by reacting a tropone cpd. (III); X is F, Cl, Br, tosyloxy or methoxy) with an aniline deriv. (III; Y is carboxyl, ester or nitrile) and (when Y is not carboxyl) subjecting the resulting intermediate to hydrolysis. In the reaction, an acid scavenger such as potassium carbonate, sodium acetate or triethylamine may be used. In addn., the reaction may be promoted by an iodide, such as sodium or potassium iodide, and Ullmann catalyt, such as active copper or copper sulphate. The reaction solvent is e.g. benzene, ethanol, t-butanol, tetrahydrofuran, acetone, dimethylsulphoxide or dimethylformamide. The reaction is at from room temp. to reflux temp., while monitoring the reaction mixt. by spectrometry observing the absorption bands around 345 nm and 405 nm which are characteristic to the anilinotropone structure.