Water‐Stable 2‐Pyridylboron Reagents: Pd‐Catalyzed 2‐Pyridylation Reaction of Aryl Halides

The stability of 2-pyridylation reagents is a long-standing issue in cross-coupling chemistry due to hydrolysis. However, as the use of pyridine-based pharmaceuticals continues to increase, there is a high demand for stable and reactive 2-pyridylation reagents. Herein, a general strategy to prepare water-stable 2-pyridylboron reagents has been developed. The application of the water-stable 2-pyridylboron reagents in a neutral Suzuki-Miyaura coupling with a halide scavenger enables an efficient 2-pyridylation reaction of aryl halides.