NEW MATERIAL:A 2-(2-aminobenzylsulfinyl)benzimidazole of formula I.
USE: Useful as an anti-ulcer agent. The compound of formula I exhibits an excellent gastric acid secretion-inhibiting action based on a specific H++K+ATPase- inhibiting action thereof.
PREPARATION: A 2-mercaptobenzimidazole of formula II is subjected to a reaction with a 2-aminobenzyl compound of formula III (X is a reactive group) preferably in the presence of an alkaline agent such as sodium hydroxide in a solvent such as toluene at the room temperature to the reflux temperature of the solution to prepare a compound of formula IV. The compound of formula IV is oxidized with an oxidizing agent such as hydrogen peroxide in an inactive solvent such as chloroform at -30°C to 50°C, especially at -15°C to 5°C, to provide the compound of formula I.
SATO MASARU
YAMAKAWA TOMIO
NOMURA YUTAKA
HAYASHI MASATOSHI