Copper-promoted dehydrosulfurative carbon-nitrogen cross-coupling with concomitant aromatization for synthesis of 2-aminopyrimidines

Copper-promoted dehydrosulfurative C-N cross-coupling of 3,4-dihydropyrimidin-1H-2-thione with amine accompanied by concomitant aromatization to generate 2-aryl(alkyl)aminopyrimidine derivatives is described. The reaction proceeded well with a wide range of thiono substrates and aryl/aliphatic amines as the coupling partners, offering efficient access to biologically and pharmacologically valuable 2-aryl(alkyl)aminopyrimidines with rapid diversification.