Ammonium salts were found to be a convenient and inexpensive reagent in the Cu- catalyzed three-component reaction with terminal alkynes and sulfonyl or phosphoryl azides leading to N-unprotected amidines. Thus obtained amidines bearing 2- bromobenzenesulfonyl moiety were efficiently cyclized by the Cu-catalyzed intramolecular N- arylation to give an important pharmacophore skeleton of 2 H-1, 2, 4-benzothiadiazine 1, ...