As drug candidates, cyclic peptides have significant therapeutic potential over other classes of peptides. For example, cyclic variants are more resistant to both exo- and endo-proteases. Therefore, in recent years, cyclic peptides have attracted an increasing amount of attention from both the scientific community and pharmaceutical companies. Multiple synthetic methods have been developed to obtain cyclic peptides; however, strategies utilizing natural amino acids in the macrocyclization are considerably limited. Recently, our group developed a strategy to harness alkyl amines as alkylating agents via C−N bond activation. We have now developed a reductive cross-coupling using pyridinium salts formed from the amino group of L-lysine’s side chain. These reactions proceed in good yields without loss of enantiomeric purity. Excitingly, this method has been advanced to a new peptide macrocyclization strategy harnessing L-lysine Katritzky pyridinium salts. The optimization and scope of these methods will be presented.<br/>

From nickel-catalyzed reductive coupling to cyclic peptide synthesis

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.