Several compounds containing amidrazone moiety are known to have interesting biological activities as anticancer, anti-inflammatory, and potent inhibitors of lipoxygenase-1. Herein we present a facile method for the regioselective synthesis of benzotriazines based on catalytic cyclization. Endowed oxidative ring closure of arylamidrazone containing compounds achieved after short treatment with CuCl2 solution. As a proof of principle, several derivatives of benzotriazines were synthesized and characterized with good purity and selectivity. Biological activity tests towards lung cancer are ongoing.