Peptide Late-Stage Diversifications by

ArticlePeptideLate-StageDiversificationsbyRhodium-CatalyzedTryptophanC7AmidationHerein,wedisclosethefirstlate-stagepeptideC–Hnitrogenationsthroughunprecedentedrhodium(III)-catalyzedpeptideC7diversification.Q8Thus,peptidesweredirectlytransformedthroughposition-selectiveC7amidationswitheasilyaccessible1,4,2-dioxazol-5-ones.StructurallycomplexpeptidesfeaturingawealthoffunctionalgroupsunderwentC7-C–Hamidationstodeliverselectivelymodifiednaturalproductanddrughybrids.WeiWang,JunWu,RosithaKuniyil,AdelinaKopp,RafaelyNascimentoLima,LutzAckermannlutz.ackermann@chemie.uni-goettingen.deHIGHLIGHTSPosition-selectivepeptidediversificationbytryptophanC7modificationLate-stagepeptideC–Nbondformation2-foldC–Hactivationforpeptidemulti-diversificationBioorthogonalmodificationoffunctionalized,structurallycomplexpeptideWangetal.,Chem6,1–12December3,2020ª2020ElsevierInc.https://doi.org/10.1016/j.chempr.2020.10.026ll