Synthesis of substituted aryl amidines from aminoacetonitriles

Aryl aminoacetonitriles are oxidized by NiO₂-H₂O or MnO₂ in the presence of a wide range of NH₂-containing compounds to afford aryl amidines, presumably via iminium intermediates. A ‘one-pot’ procedure for the preparation of heteroaryl amidines from N-containing heteroaryl halides through a process comprising sequential S_NAr substitution and oxidation has also been developed.