AROMATIC ACETYLENECARBOXYLIC ACID AMIDE DERIVATIVE AND ITS PREPARATION

NEW MATERIAL:A compound shown by the formula I (Y is OH, or lower alkoxyl; R is H, or lower alkyl). EXAMPLE:3-(3,4-Dimethoxyphenyl)-N-(2-carboxyphenyl)propionic acid amide. USE:An antispasmodic. Having a relaxing action on smooth muscle, useful for spastic pain in various digestive organ disorder such as gastric ulcer, duodenal ulcer, gastritis, enteritis, cholecystitis, gallstone disease, biliary dyskinesia, etc. Also useful for remedying bronchial asthma, hypertension, etc. PREPARATION:A novel dihalogen compound shown by the formula II (X1 and X2 are halogen) is dehydrohalogenated in the presence of a basic substance (e.g., 1,5-diazabicyclo[3,4,0]-5-nonene) in an inert organic solvent such as dimethyl sulfoxide, etc. at 50-70 deg.C, and, if necessary, it is hydrolyzed to give a compound shown by the formula I .