Abstract

β-Aryl ketones are present in various natural products and bioactive molecules. Till now, -aryl ketone has been synthesized through the directing group (DG) approach or Mizoroki-Heck coupling. Herein, we reported a palladium(II) catalyzed dual ligand-enabled non-directed C−H alkylation with arene and heteroarene as a limiting reagent for the synthesis of -(hetero)aryl ketones. The combined influence of 2-methyl quinoxaline and N-acetyl phenylalanine ligands imparts complementary selectivity, facilitating the diversification of drugs and natural products through C−H alkylation. Integrated experimental and computational mechanistic studies demonstrate the C−H activation as both the regio- and rate-determining step. Interestingly, while the Pd−Ag heterobimetallic species is not directly involved in the 1,2-migratory insertion step, it is proposed to play a vital role during the product release phase of the catalytic cycle.

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