N-alkyl formamide activation by using of copper/oxidant system via tandem/domino reaction pathway to construct CÀ N/CÀ O bond formation is reported. This protocol elucidated a method for the synthesis of pharmaceutically interested 3-alkyl-1,3benzoxazine-2,4-dione and 1,3-methylene-3-alkylbenzoxazine-2-one derivatives without the aid of toxic chemicals such as phosgene or its derivatives.