Adebomi V,
Cohen RD,
Wills R,
Chavers HA. H,
Martin GE,
Raj M.
* Auburn University, USA
CyClick Chemistry for the Synthesis of Cyclic Peptides.
Angew. Chem. Int. Ed. 2019;
58: 19073-19080
Key words
click chemistry - peptides - macrocycles - stereoselectivity
Significance
The pharmaceutical industry’s interest in peptide therapeutics is increasing owing to their low toxicities, high specificities towards targeted proteins, and so on. The authors describe a stereoselective macrocyclization of peptides through click chemistry.
Comment
This DMAP-mediated intermolecular cyclization gives the desired cyclic peptides in moderate to high yields without the formation of linear oligopeptides through intramolecular reactions.
