Free amino group-directed C(sp2)–H arylation of α-amino-β-aryl esters by palladium catalysis

Native amino-directed palladium-catalyzed C(sp3)–H activation/functionalization has been developed for modification of α-amino acids and peptides. Herein a palladium(II)-catalyzed C(sp2)–H arylation of α-amino-β-aryl esters has been disclosed, using the native amino as the directing group. A variety of chiral α-amino-β-aryl esters can be functionalized to give the corresponding ortho-substituted mono- and di-arylated products.