New benzochiazo - ru and benzuimidazo - the ru derivative and designates those as the active ingredient the anti- ulcer medicine

摘要

NEW MATERIAL:A compound of formula I [X is S or NH; R1 is H, lower alkoxy, Cl, Br or I; R2 is H, (substituted) lower alkyl, vinyl, aryl or acyl; m and n are 0-2]. EXAMPLE:5-Chloro-2-[(2-ethoxyethyl)sulfinyl]benzothiazole. USE:A drug. An active ingredient for anti-ulcer agents. The compound has a strong gastric acid-secreting action and an excellent gastric mucosa-protecting action and is effective for treating and preventing gastric ulcer and duodenal ulcer. PREPARATION:For example, a compound of formula II is reacted with a compound of formula III (Y is halogen, tosyloxy, mesyloxy, etc.) in a solvent such as N,N-dimethylamide in the presence of NaH, etc., to provide the compound of formula I wherein n is 0. The compound of formula I is reacted with 1-1.2mol equivalent of an oxidizing agent such as H2O2 in the presence of a catalyst such as sodium tungstate to provide the compound of formula I wherein n is 1.