BODIPY Peptide Labeling by Late‐Stage C(sp3)−H Activation

: Late-stage BODIPY diversification of structurally complex amino acids and peptides was accomplished by racemization-free palladium-catalyzed C(sp3 )-H activation. Transformative fluorescence modification proved viable by triazole-assisted C(sp3 )-H arylation in a chemo- and site-selective fashion, providing modular access to novel BODIPY peptide sensors.