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

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.