AMINOSTYRIL COMPOUND AND LEUKOTRIENE ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT

摘要

NEW MATERIAL:A compound of formula I (A is a linking group of 3-4 atoms; B is 5-6-membered substituted, unsubstituted heterocyclic group residue containing 1-2 hetero atoms, naphthyl, 5-7C alkyl) and its salt. EXAMPLE:2-[trans-3-(3-Carboxypropanamide)styryl]quinoline. USE:Leukotriene antagonist. PREPARATION:The reaction of a compound of formula II with an omega- halocarboxylic acid ester of formula III (X is halogen) is carried out in the presence of an organic base such as triethylamine or pyridine in a solvent such as aromatic hydrocarbon ether or halogenated hydrocarbon, at 0oC to the boiling point of the solvent to effect N-alkylation whereby the compound of formula IV is obtained. The product is hydrolyzed in an aqueous alcohol using an alkali metal inorganic base, and treated with a mineral acid to give the compound of formula I.