NOVEL GUANIDINOMETHYLBENZOIC ACID DERIVATIVE AND REMEDY FOR PEPTIC ULCER CONTAINING SAID DERIVATIVE

摘要

NEW MATERIAL:A derivative expressed by formula I (R1 is H, halogen or lower alkyl; R2 is H or lower alkoxy) or acid addition salt thereof. EXAMPLE:O-Benzylsalicyl 4-guanidinomethylbenoate. USE:A remedy for peptic ulcer useful as a medicine having high remedial effects with hardly any side effects. PREPARATION:A 4-guanidinomethylbenzoic acid expressed by formula II is reacted with phenols expressed by formula III in the presence of a condensing agent, such as dicyclohexylcarbodiimide, to afford the aimed compound expressed by formula I. The reaction is preferably carried out in a solvent, such as DMF, pyridine or toluene, at room temperature - 140 deg.C for 30min-24 hr. The compound expressed by formula II is obtained by amidinating p- aminomethylbenzoic acid with S-methylisothiourea.