Benzothiadiazine dioxide (II) was prepared by cyclization of methyl anthranylate (I) with sulfamoyl chloride, followed by aqueous NaOH. After silylation of (II) by means of hexamethyldisilazane, alkylation with benzyloxymethyl acetate (III) in the presence of boron trifluoride etherate produced the 3-(benzyloxymethyl)benzothiazine (IV). Further alkylation of (IV) with benzyl bromide in aqueous NaHCO3 furnished the title compound.