Late-stage construction of stapled peptides through Fujiwara-Moritani reaction between tryptophan and olefins.

Herein, the first example of a palladium-catalyzed Fujiwara-Moritani reaction for olefination of tryptophan (Trp) residues, free from directing groups, was presented. The developed reaction proceeds efficiently for peptide modification, ligation and peptide stapling.