Microwave assisted water mediated benzylic C–H functionalization of methyl aza-arenes and nucleophilic addition to aromatic aldehydes

A highly efficient method is described for the sp3 C–H bond functionalization of methyl aza-arenes in the presence of water under microwave irradiation and subsequent addition to aromatic aldehydes. This transformation represents an efficient way to synthesize 2-alkyl aza-arene derivatives from simple starting materials.