Palladium-catalyzed direct ortho-acylation through an oxidative coupling of acetanilides with toluene derivatives.

A facile ortho-acylation of acetanilides by a Pd-catalyzed oxidative C-H activation was developed in which low toxic, stable, and commercially available toluene derivatives were first used as acylation reagents by a tandem reaction to form o-acylacetanilides with moderate to good yields. Inexpensive, safe, and environmentally benign TBHP was proved to be an effective oxidant for these transformations.