Peptide Macrocyclization Through Palladium-Catalyzed Late-Stage C-H Activation.

Abstract

Cyclic peptides are an important class of bioactive compounds for the chemical biology and pharmaceutical industry. Chemical synthesis of highly constrained cyclic peptides is often challenging. Here we describe the synthetic strategy of peptide macrocyclization through late-stage palladium-catalyzed C-H activation. These methods utilize endogenous backbone amides in the peptide sequence as directing groups and are efficient in the preparation of small-to-middle size peptide macrocycles.