Site-Selective Derivatization and Cyclization of Peptides by On-Resin Metal-Catalyzed C-H Activation.

This research project aims at developing innovative procedures for the derivatization of oligopeptides. It combines on-resin multicomponent reactions, peptide couplings and metal-catalyzed C-C bond forming reactions, into an effective methodology for the site-selective derivatization of solid-supported (pseudo)peptides. Three main solid-phase protocols will be developed: site-selective arylation of peptides by Pd-catalyzed C-H activation using traceless directing groups as N-substituents of the neighboring amide, macrocyclization of peptide side chains using Pd-catalyzed C-H activation procedures of dehydroalanine-containing peptides and similars, and intramolecular Pd (II)-catalyzed C-H arylation of peptides leading to indolo-peptides.

Keywords:peptides

Disciplines:Analytical chemistry, Physical chemistry, Organic chemistry, Condensed matter physics and nanophysics, Pharmaceutical analysis and quality assurance, Inorganic chemistry