ANILINE DERIVATIVE, ITS PREPARATION, AND DRUG CONTAINING SAME AS ACTIVE INGREDIENT

摘要

NEW MATERIAL:A compound shown by the formula I (R<1> is 1-15C alkyl, alkoxy, 2-15C alkenyl, phenyl, benzyl, etc.; R<2> and R<2>' are H, or 1-20C alkyl; R<3> is carboxy, 2-6C alkoxycarbonyl, mercapto, etc.; R<4> and R<5> are H, halogen, 1- 4C alkyl, alkoxy, etc.; n is 0-2; dotted line part is double bond or single bond). EXAMPLE:N-(P-Amylcinnamoyl)-3-chloroanthranilic acid. USE:A leukotriene antagonist. A phospholipase inhibitor. A 5alpha-reductase inhibitor. Useful for remedying allergic diseases, prostatic hypertrophy, alopecia, thrombosis, etc. PREPARATION:An acid chloride shown by the formula II is reacted with an amine shown by the formula III in an inert organic solvent in the presence of a tertiary amine (e.g., triethylamine or pyridine) at -20-40 deg.C preferably at 0 deg.C- room temperature to give a compound shown by the formula I .