Late‐Stage Peptide Diversification by Bioorthogonal Catalytic CH Arylation at 23 °C in H2O |
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| Authors: | Dr Yingjun Zhu Michaela Bauer Prof Dr Lutz Ackermann |
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| Affiliation: | Institut für Organische und Biomolekulare Chemie, Georg‐August‐Universit?t, Tammanstrasse 2, 37077 G?ttingen (Germany) http://www.org.chemie.uni‐goettingen.de/ackermann/ |
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| 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. |
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| Keywords: | C H activation chemoselectivity H2O late‐stage derivatization peptides |
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