One-Pot Directed Metallation-Coupling Reactions of Pyridine Derivatives

Significance

Substituted aza-biaryls are useful synthetic intermediates in the preparation of various biologically relevant molecules. The authors developed a one-pot protocol for the directed metallation-borylation-cross-coupling reaction for a broad number of functionalized pyridines. In some cases, the intermediate pinacolboronic esters could be isolated. Alternatively, a one-pot oxidation of the boronate into the phenol can be performed. A profound literature survey, concerning the preparation and the use of various pyridyl boronates is given.