Rhodium‐Catalyzed Regioselective C7Ar‐Functionalization of Tryptophan with Quinones and its Late Stage Peptide Exemplification

Abstract Pivaloyl‐directed Rh(III)‐catalyzed regioselective C7 Ar ‐H functionalization of protected tryptophans were accomplished with 1,4‐benzoquinones, furnishing a series of quinone‐appended tryptophan‐based unnatural amino acids in high yields. Further, the late stage functionalization on tryptophan‐containing dipeptides was achieved with 1,4‐benzoquinones in moderate reactivity.