Late-Stage Peptide Macrocyclization by Palladium-Catalyzed Site-Selective C-H Olefination of Tryptophan.
Angew Chem Int Ed Engl
; 59(34): 14686-14692, 2020 08 17.
Article
em En
| MEDLINE
| ID: mdl-32511858
ABSTRACT
Transition-metal-catalyzed C-H activation has shown potential in the functionalization of peptides with expanded structural diversity. Herein, the development of late-stage peptide macrocyclization methods by palladium-catalyzed site-selective C(sp2 )-H olefination of tryptophan residues at the C2 and C4 positions is reported. This strategy utilizes the peptide backbone as endogenous directing groups and provides access to peptide macrocycles with unique Trp-alkene crosslinks.
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MEDLINE
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En
Ano de publicação:
2020
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Article