Copper-catalyzed oxidative three-component synthesis of N, N',N″-trisubstituted guanidines.

A copper-catalyzed three-component synthesis of trisubstituted N-aryl guanidines involving cyanamides, arylboronic acids, and amines has been developed. This operationally simple oxidative process, which is performed in the presence of K2CO3, a catalytic amount of CuCl2·2H2O, bipyridine, and oxygen (1 atm), allows the rapid assembly of N,N',N″-trisubstituted aryl guanidines.