Abstract

AbstractSecondary C(sp3)−H arylations were accomplished by palladium catalysis with triazoles as peptide bond isosteres. The unique power of this approach is highlighted by the possibility of achieving secondary C(sp3)−H functionalizations on terminal peptides as well as the unprecedented positional‐selective C(sp3)−H functionalization of internal peptide positions, setting the stage for modular peptide late‐stage diversification.

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