Click Chemistry as a Macrocyclization Tool in the Solid-Phase Synthesis of Small Cyclic Peptides
2007; American Chemical Society; Volume: 9; Issue: 24 Linguagem: Inglês
10.1021/ol702228u
ISSN1523-7060
AutoresRushia Turner, Allen G. Oliver, R. Scott Lokey,
Tópico(s)Monoclonal and Polyclonal Antibodies Research
ResumoDespite the vast number of techniques developed for the cyclization of small peptides, cyclization efficiency remains problematic in peptides that lack turn-promoting structures. Here we demonstrate the utility of click chemistry as a macrocyclization tool in the solid-phase synthesis of cyclic tetra-, penta-, hexa-, and heptapeptides. On-resin cyclization is completed at room temperature within 6 h, resulting in predominantly monomer with small amounts of cyclomultimer byproducts.
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