Synfacts 2019; 15(11): 1323
DOI: 10.1055/s-0039-1619006
Peptide Chemistry
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Cyclic and Bicyclic Peptides

Hisashi Yamamoto
Wataru Muramatsu
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
Further Information

Publication History

Publication Date:
18 October 2019 (online)



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.



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.