Ru?Catalyzed C?H Hydroxylation of Tyrosine?Containing Di? and Tripeptides toward the Assembly of L?DOPA Derivatives

The development of catalytic tools for the late-stage modification amino acids within a peptide framework is challenging task capital importance. Herein, we report Ru-catalyzed C(sp2)?H hydroxylation collection Tyr-containing di- and tripeptides featuring use carbamate as removable directing group PhI(OCOCF3)2 (PIFA) oxidant. This air-compatible tagging technique reliable, scalable provides access to L-DOPA (L-3,4-dihydroxyphenylalanine) peptidomimetics in racemization-free fashion. Density Functional Theory calculations support Ru(II)/Ru(IV) cycle.