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Published on: August 19, 2012
Late-Stage Peptide Diversification by Bioorthogonal Catalytic C-H Arylation at 23 °C in H2 O
Yingjun Zhu1, Michaela Bauer1, Lutz Ackermann2
1Institut für Organische und Biomolekulare Chemie, Georg-August-Universität, Tammanstrasse 2, 37077 Göttingen (Germany) http://www.org.chemie.uni-goettingen.de/ackermann/
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 H2 O.
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