| 摘要 |
PURPOSE:To obtain the titled compound useful as pharmaceuticals, in one step and high yield, by reacting 2-methoxy-5-sulfamoylbenzoic acid directly with 1- ethyl-2-aminomethylpyrrolidine using diethyl cyanophosphate as a catalyst. CONSTITUTION:The objective 2-methoxy-5-sulfamoylbenzoyl-(N-ethyl)-2-pyrrolidinemethylamine of formula VI can be prepared by reacting the easily available or producible 2-methoxy-5-sulfamoylbenzoic acid of formula I with 1-ethyl-2- aminomethylpyrrolidine of formula II at room temperature, using diethyl cyanophosphate of formula III as a catalyst. EFFECT:The objective compound can be prepared in a short time under extremely advantageous condition.
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