Some 2-sulfamoylmethylbenzoxazole derivatives were synthesized from 2-bromomethylbenzoxazole by reaction with sodium bisulfite, followd by chlorination and amination. Among them, 2-sulfamoylmethylbenzoxazole (5a) showed the strongest anticonvulsant activity, which was compared with that of 3-sulfamoylmethyl-1, 2-benzisoxazole (I).