Synthesis of 1,2-dihydro-1,3,5-triazine derivatives via Cu(II)-catalyzed C(sp3)-H activation of N,N-dimethylethanolamine with amidines.

1,2-Dihydro-1,3,5-triazines and symmetrical 1,3,5-triazines were obtained in up to 81% yields from amidines and N,N-dimethylethanolamine catalyzed by CuCl2. The reaction involves three C-N bond formations during the oxidative annulation process and the mechanism was proposed. This efficient synthesis of 1,2-dihydro-1,3,5-triazines was developed for the first time.