Palladium-catalyzed β-acyloxylation of simple amide via sp3 C-H activation.

β-Acyloxy amides are prepared in moderate to high yields by palladium-catalyzed acyloxylation of primary sp(3) C-H bonds from simple amides without any special directing group. A catalytic system of Pd(OAc)2/CF3CO2H/K2S2O8 is available to various amides with N-substituted by linear alkanes, cyclic alkanes, and electron-deficient benzyl compounds in this reaction. Acyloxylated products could be transformed easily to the corresponding β-hydroxy amides.