Abstract
Herein, we report a palladium-catalyzed C(sp2)-H di- or monoarylation of short peptides containing N-terminal benzamide groups using aspartic acid (Asp) as an endogenous directing group. This strategy has the following merits: a broad substrate scope, selective diarylation of peptides, and gram-scale synthesis. Furthermore, this strategy can be successfully utilized to synthesize peptide-peptide conjugates.
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