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

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