A domino S–N and C–N coupling/oxidative aromatization process to synthesize 2-aminothio-phenylpyrimidines and 2-amino-phenylpyrimidines by S–N and C–N cross-coupling reactions is described. This methodology couples 3,4-dihydropyrimidine-2-thiones and secondary amines catalyzed by molecular iodine. Remarkably the C–N coupled product was obtained via a desulfitative coupling-aromatization reaction in one-pot reaction.
