Zhang Y,
Zhang Q,
Wong CT. T,
Li X.
* The University of Hong Kong, P. R. of China
Chemoselective Peptide Cyclization and Bicyclization Directly on Unprotected Peptides.
J. Am. Chem. Soc. 2019;
141: 12274-12279
Key words
cyclic peptides - directing groups - phthalaldehyde
Significance
Due to their unique properties, cyclic peptides and their synthesis have received
considerable attention from medicinal chemists. The authors have developed an ortho-phthalaldehyde-guided chemoselective cyclization of unprotected peptides.
Comment
This cyclization reaction for the synthesis of cyclic and bicyclic peptides is guided
successfully by ortho-phthalaldehyde. The target compounds are obtained in high conversion yields with
excellent chemoselectivity.
