BENZIMIDAZOLE DERIVATIVE, PRODUCTION THEREOF AND ANTIULCER AGENT CONTAINING SAME

摘要

NEW MATERIAL:The benzimidazole derivative of formula I (R1 is cycloalkyl, phenyl or aralkyl; R2 is H or lower alkyl; R1 and R2 may together with adjacent N atom form a ring). EXAMPLE:2-(2-Piperidinobenzylsulfinyl)benzimidazole. USE:It has excellent effect to suppress the gastric juice secretion by the specific H1+K<+>ATPase-inhibiting action and is useful as an antiulcer agent which can be administered orally or parenterally. PREPARATION:The compound of formula I can be produced by (1) reacting the 2-mercaptobenzimidazole compound of formula II with the 2-aminobenzyl compound of formula III (X is reactive group) in an inert solvent such as acetone at a temperature between room temperature and the refluxing point and (2) oxidizing the resultant compound of formula IV with an oxidizing agent such as hydrogen peroxide in an insert solvent such as chloroform at -15-+5 deg.C.