Peptide Modification via N‑Terminal-Residue-Directed γ‑C(sp3)–H Arylation
Postassembly modification of peptides via C(sp3)–H functionalization provides an efficient way to prepare functionalized peptides for biological study and pharmaceutical development. In this work, we developed a new method for γ-C(sp3)–H functionalization of aliphatic side chains of N-terminus-unp...
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Veröffentlicht in: | Organic letters 2020-11, Vol.22 (21), p.8692-8696 |
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Hauptverfasser: | , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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Zusammenfassung: | Postassembly modification of peptides via C(sp3)–H functionalization provides an efficient way to prepare functionalized peptides for biological study and pharmaceutical development. In this work, we developed a new method for γ-C(sp3)–H functionalization of aliphatic side chains of N-terminus-unprotected peptides. With the N-terminal residues as directing groups, a wide range of di-, tri-, tetra-, and pentapeptides underwent C–H arylation of the residues (Val, Ile, Tle) at the +2 position from the N-terminus. |
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ISSN: | 1523-7060 1523-7052 |
DOI: | 10.1021/acs.orglett.0c03279 |