Catalytic Asymmetric Activation of a CH Bond Adjacent to a Nitrogen Atom: A Versatile Approach to Optically Active α‐Alkyl α‐Amino Acids and C1‐Alkylated Tetrahydroisoquinoline Derivatives

Simple and efficient: A one-pot oxidative and catalytic enantioselective alkylation of α-CH bonds adjacent to a nitrogen atom was realized for the first time. This novel strategy provides a simple, efficient, and environmentally friendly access to diverse optically active α-alkyl α-amino acid and C1-alkylated tetrahydroisoquinoline derivatives.