Synthesis of Unsymmetrical Urea Derivatives via Cu‐Catalyzed Reaction of Acylazide and Secondary Amine

The synthesis of unsymmetrical urea generally requires toxic reagent, solvent and harsh reaction condition. Herein, we introduce Cu-catalyzed greener and safer unsymmetrical urea derivatives synthesis in ethyl acetate. This method minimized utilization of toxic reagent. A variety of indole, amines, and azides with bis-indole successfully employed leading to high yields and gram scale synthesis of isolated urea.