Abstract

AbstractThe multicomponent assembly of the 2‐(methylthio)‐aniline (MTA) directing group in N‐methylated Ugi 4‐CR adducts using the (2‐isocyanophenyl)(methyl)sulfane and the subsequent Pd(II)‐mediated mono‐selective β‐C(sp3)−H bond activation process have been successfully developed for the synthesis of arylated amino acids and peptide systems.

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