Cu-Catalyzed [3 + 3] Annulation for the Synthesis of Pyrimidines via β‑C(sp3)–H Functionalization of Saturated Ketones

A novel, efficient, and facile approach for the synthesis of structurally important pyrimidines has been successfully developed by Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones. This method provides a new protocol for the synthesis of pyrimidines by a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization via direct β-C­(sp3)–H functionalization of saturated ketones followed by annulation with amidines.