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Late‐Stage Peptide Diversification by Bioorthogonal Catalytic CH Arylation at 23 °C in H 2 O
Author(s) -
Zhu Yingjun,
Bauer Michaela,
Ackermann Lutz
Publication year - 2015
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201501831
Subject(s) - bioorthogonal chemistry , catalysis , chemistry , palladium , peptide , tryptophan , surface modification , combinatorial chemistry , stage (stratigraphy) , stereochemistry , organic chemistry , biochemistry , biology , amino acid , click chemistry , paleontology
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 H 2 O.