Ueda A,
*,
Makura Y,
Kakazu S,
Kato T,
Umeno T,
Hirayama K,
Doi M,
Oba M,
Tanaka M.
*
Nagasaki University, Japan
E-Selective Ring-Closing Metathesis in α-Helical Stapled Peptides Using Carbocyclic α,α-Disubstituted α-Amino Acids.
Org. Lett. 2022;
24: 1049-1054
Key words
cyclic peptides - ring-closing metathesis - stereoselectivity - peptide stapling
Significance
Cyclopeptides are key moieties widely present in a number of bioactive products, including some with clinical applications. The authors developed ring-closing metathesis in α-helical stapled peptides.
Comment
The ring-closing metatheses of α-helical stapled peptides containing leucine or valine residues proceeded in moderate to high yields, generally in an E-selective manner.
