PREPARATION OF N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-2- METHOXY-5-SULFAMOYLBENZAMIDE

摘要

PURPOSE:To prepare the titled compound under mild conditions, in high yield, by using the easily available (N'-tosyl)-2-methoxy-5-sulfamoylbenzohydrazide as an intermediate, and reacting the intermediate with 1-ethyl-2-aminomethylpyrrolidine in the presence of an oxidizing agent. CONSTITUTION:N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfamoylb enzamide of formula V can be prepared by using (N'-tosyl)-2-methoxy-5-sulfamoylbenzohydrazide of formula III as an intermediate, and reacting the intermediate with 1-ethyl-2-aminomethylpyrrolidine in the presence of an oxidizing agent (e.g. lead tetraacetate). The reaction proceeds at room temperature in a short time without side reactions. The compound of formula III used as the intermediate can be obtained by the reaction of 2-methoxy-5-sulfamoylbenzohydrazide of formulaIwith 4-methylbenzenesulfonyl chloride of formula II. USE:Antiulcer agent, antidepressant, etc.