Cu-Catalyzed intermolecular [3+3] annulation involving oxidative activation of an unreactive C(sp3)-H bond: access to pyrimidine derivatives from amidines and ketones

A facile and efficient approach for the synthesis of various pyrimidine derivatives from amidines and ketones via a Cu-catalyzed intermolecular oxidative coupling process using TEMPO/O-2 as a co-oxidant has been developed. This novel protocol features unreactive C(sp(3))-H bond amination, a wide range of substrates, good functional group tolerance and mild reaction conditions.