84. Late-Stage Diversification of Peptides via Pd-Catalyzed SiteSelective δ‑C(sp2)‑H Fluorination and Amination

Tang, J.;* Lu, F.; Sun, Y.; Zhang, G.; Zhang, E.; Jiang, Y.-Y. J. Org.Chem. 2023, 88, 14165-14171. Download Link.

Abstract: Site-selective C−H fluorination is an attractive strategy for directly transforming inert C−H bonds into C−F bonds, yet it remains a significant challenge. Herein, we have developed an efficient and versatile strategy for site-selective fluorination and amination of phenylalanine-containing peptides via late-stage Pd-catalyzed δ-C(sp2)-H activation, providing a valuable tool for the in situ synthesis of fluorinated indoline scaffolds within peptides.