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Copper-promoted dehydrosulfurative C-N cross-coupling of 3,4-dihydropyrimidin-1-2-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.

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An aerobic Cu-promoted oxidative dehydrosulfurative carbon-oxygen cross-coupling of 3,4-dihydropyrimidin-1-2-thiones (DHPMs) with both aliphatic and aromatic alcohols is described. Together with the ready availability of DHPMs and both alcohols, the method furnishes facile access to biologically valuable 2-alkoxypyrimidines with rapid diversification.

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