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

Abstract

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.