Direct Oxidative Arylation of Aryl CH Bonds with Aryl Boronic Acids via Pd Catalysis Directed by the N,N‐Dimethylaminomethyl Group

Biaryl skeletons were directly constructed via palladium-catalyzed ortho-arylation of N,N-dimethyl benzylamine with aryl boronic acids with high efficiency and high regioselectivity under open-flask conditions. The N,N-dimethylaminomethyl group was first applied as a directing group in such an oxidative coupling. Various substrates proved to be efficient coupling partners, furnishing the corresponding ortho-monoarylated or -diarylated arenes in moderate to good yields under mild conditions.