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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. [ABSTRACT FROM AUTHOR]

A palladium catalyzed selective C(sp3)–H arylation and acetoxylation of alcohols using a practical bidentate auxiliary were developed. Masked alcohols were selectively arylated at the β-position with diverse aryl iodides for the first time. Moreover, an efficient and site-selective acetoxylation of various primary methyl, methylene, and benzylic C(sp3)–H bonds was performed by using cheap K2S2O8 as the external oxidant. [ABSTRACT FROM AUTHOR]