Late‐Stage Peptide Diversification by Bioorthogonal Catalytic C-H Arylation at 23 °C in H2O

Abstract

The step-economical late-stage diversification of tryptophan-containing peptides was accomplished through chemo- and site-selective palladium-catalyzed CH arylation under exceedingly mild reaction conditions. Thus, the CH functionalization occurred efficiently at 23 °C with a catalyst loading as low as 0.5 mol %, and/or in H₂O.