Palladium‐Catalyzed Regioselective Acylation of Diazines with Toluenes: A New Approach to the Synthesis of ortho‐Diacylbenzenes

A highly efficient and practical procedure for chemo- and regioselective synthesis ofortho-diacylbenzenes through Pd-catalyzed oxidative C-H bond activation has been developed. Using this method, a variety ofortho-diacylbenzenes were prepared in moderate to good yields, by direct acylation of diazines with toluene derivatives as acylation source.Ortho-diacylbenzenes may be used as precursors in synthesis of pharmaceuticals and agrochemicals.