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Late-Stage Functionalization of Histidine in Unprotected Peptides

Noisier, Anaïs F. M; Johansson, Magnus J.; Knerr, Laurent; Hayes, Martin A.; Drury, William J.; Valeur, Eric; Malins, Lara; Gopalakrishnan, Ranganath


The late‐stage functionalization (LSF) of peptides represents a valuable strategy for the design of potent peptide pharmaceuticals by enabling rapid exploration of chemical diversity and offering novel opportunities for peptide conjugation. While the C(sp2)−H activation of tryptophan (Trp) is well documented, the resurgence of radical chemistry is opening new avenues for the C−H functionalization of other aromatic side‐chains. Herein, we report the first example of LSF at C2 of histidine (His)...[Show more]

CollectionsANU Research Publications
Date published: 2019
Type: Journal article
Source: Angewandte Chemie
DOI: 10.1002/anie.201910888


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