Pd-catalysed β-selective C(sp3)–H arylation of simple amides

Abstract

An efficient Pd-catalysed β-C(sp³)–H arylation of diverse native amides with aryl iodides was developed. This protocol overcomes the necessity of the Thorpe–Ingold effect and features broad substrate scope and good functional group tolerance. The potential application of this protocol is collectively demonstrated by gram-scale synthesis and the synthesis of several bioactive molecules.