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Updated: Sep 24, 2025

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
Selective Stepwise Arylation of Unprotected Peptides by PtIV Complexes
Xiaoxi Lin1, Elvira Haimov2, Boris Redko2
1School of Chemistry, The Sackler Faculty of Exact Sciences, Tel Aviv University, Tel Aviv, 69978, Israel.
Abstract:
LPtIV F(Aryl) complexes bearing a bulky bidentate 2-[bis(adamant-1-yl)phosphino]phenoxide ligand (L) demonstrate excellent reactivity and selectivity in the arylation of X-H (X=S, N) bonds of amino acid residues in unprotected peptides under mild, including aqueous, conditions. Stepwise addition of these complexes allowed a convenient one-pot introduction of different aromatic groups in the X-H bonds of Cys and N terminus. PtIV reagents can also be used to further arylate N-H bonds in Lys and Trp providing access to peptides bearing multiple aromatic groups.
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