Journal
ORGANIC LETTERS
Volume 9, Issue 24, Pages 5011-5014Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol702228u
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- NCI NIH HHS [CA104569-03] Funding Source: Medline
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Despite 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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