Copper-Catalyzed N-Alkyl Formamide Activation: Tandem Oxidative Coupling Approach for the Construction of C-N and C-O Bonds to Synthesize 3-Alkyl-1,3-Benzoxazine-2,4-Dione and 4-Methylene-3-Alkyl-1,3-Benzoxazine-2-One Derivatives

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

Automated summary

This study reports a method for the synthesis of pharmaceutically interested compounds by activating N-alkyl formamide using a copper/oxidant system via a tandem/domino reaction pathway to construct C-N/C-O bond formation, without the need for toxic chemicals.