Palladium-Catalyzed Late-Stage Macrocyclization for the Synthesis of Cyclophane-Braced Glycopeptides

Keywords

late-stage functionalization - palladium catalysis - macrocyclization - glycopeptides

Significance

Macrocyclic peptides have gained tremendous attention in peptide drug discovery. In this article, the authors have developed a palladium-catalyzed macrocyclization by selective C(sp³)–H arylation of the anomeric bonds for the synthesis of cyclophane-braced glycopeptides.

Comment

A series of macrocyclic cyclophane-braced glycopeptides has been synthesized in good to moderate yields by a palladium-catalyzed site-selective anomeric C(sp³)–H cyclization approach. This protocol showcases the efficiency of a palladium-catalyzed C–H activation strategy for the synthesis of unnatural cyclic peptides.

Publication History

Article published online:
28 January 2025