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Efficient Construction of Proline-Containing β‑Turn Mimetic Cyclic Tetrapeptides via CuAAC Macrocyclization

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posted on 15.03.2013, 00:00 authored by Gagan Chouhan, Keith James
A range of macrocyclic β-turn mimetic tetrapeptides was prepared by efficient copper-tris(triazole) ligand complex catalyzed azide–alkyne “click” macrocyclizations in good to high yields. Preliminary conformational studies using X-ray crystallography and NMR spectroscopy demonstrated the presence of intramolecular H-bonds characteristic of β-turns in these cyclic tetrapeptides.