This method enables site-selective C(sp2)-H amination and olefination in phenylalanine, highlighting diverse applications.
Herein, we report Pd-catalyzed and site-selective C(sp2)-H amination/olefination of phenylalanine. The transformation proceeds via a troponyl carbonyl-directed intramolecular C-N cyclization forming indoline scaffolds through C(sp2)-H activation with PIDA. In the absence of PIDA, ortho-C(sp2)-H olefination occurs at phenylalanine. This method shows broad substrate scope and excellent functional group tolerance, providing a versatile tool for peptide diversification.
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Nayak et al. (2025) studied this question.
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