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Updated: May 2, 2026

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
Published on: September 28, 2022
Cyclic carbo-isosteric depsipeptides and peptides as a novel class of peptidomimetics
Stéphanie M Guéret1, Peter Meier, Hans-Jörg Roth
1Global Discovery Chemistry, Novartis Institutes for Biomedical Research , Novartis International AG, Postfach, CH-4002 Basel, Switzerland.
Abstract:
A novel and highly efficient cyclization method has been developed to access a new class of cyclic carbo-isosteric depsipeptides and carbo-isosteric peptides. Our strategy requires easily accessible C-terminal methyl ketone ester or amide functionalized linear precursors as starting materials. The well-known reductive amination has then been used to afford cyclic tetra- to octa-pseudopeptides via a selective intramolecular formation of a glycine peptidomimetic unit under moderate dilution.
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