On-resin Cα-functionalization of N-arylglycinyl peptides with boronic acids

Abstract

A late-stage α-C–H functionalization reaction of resin-bound, electron-rich N-aryl peptides with boronic acid nucleophiles under mild conditions is reported. We explore the impact of the N-arylglycinyl peptide structure on reactivity, and present a scope of the optimized reaction where both the peptide sequence and nature of boronic acid derivatives are varied.