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Zhu, Yingjun; Bauer, Michaela; Ackermann, Lutz
Chemistry : a European journal, July 6, 2015, Letnik: 21, Številka: 28Journal Article
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 °C with a catalyst loading as low as 0.5 mol %, and/or in H2O. CH arylation of oligopeptides was achieved in aqueous media under exceedingly mild reaction conditions. The chemo‐ and site‐selective nature of the late‐stage diversification protocol illustrates the potential of our strategy for peptide ligation and fluorescence labeling (see scheme).
