Palladium-Catalyzed Selective C-H Benzylation towards Functionalized Azoles with a Quaternary Carbon Center

The direct C?H benzylation of azoles with benzyl chlorides proceeds efficiently, via sequential cleavage of one sp2 C?H bond and two sp3 C?H bonds in the presence of a palladium catalyst, to generate a wide range of tribenzylated azoles with a quaternary carbon center efficiently. The same catalyst could also promote the mono- and di-benzylation reactions through fine turning of the base and reaction conditions.