Nickel-Catalyzed ortho-C-H Thiolation of N-Benzoyl α-Amino Acid Derivatives

We developed the first nickel-catalyzed direct ortho-thiolation of N-benzoyl alpha-amino acid derivatives. This novel strategy showed wide generality, functional tolerance, and high regioselectivity. In addition, dipeptide derivatives were also compatible with this transformation system, providing a potential protocol for the direct modification of peptide derivatives.