| 摘要 |
NEW MATERIAL:A compound expressed by formula I (R is 1-10C alkyl which may be substituted by alkenyl, aryl, cyano, OH alkoxycarbonyl or aminocarbonyl) and salt thereof. EXAMPLE:2-Methylthio-1-(2-pyridylmethyl)benzimidazole. USE:A remedy for peptic ulcer having inhibitory effect on gastric acid secretion and protective action on gastric mucosae with low toxicity. PREPARATION:For example, an imidazole derivative expressed by formula II is reacted with 2-picolyl chloride expressed by formula III in the presence of a base, e.g. sodium hydride, etc., in an organic solvent, e.g. DMF, etc., at room temperature - 80 deg.C to give a sulfide compound in the compound expressed by formula I. the resultant compound is then reacted with one equivalent oxidizing agent, e.g. m-chloroperbenzoic acid, etc., in a solvent to afford the aimed sulfinyl compound. When the aobve-mentioned sulfide compound is reacted with 2 equivalents oxidizing agent, the aimed sulfonyl compound is obtained. |
