Water-Stable 2-Pyridylboron Reagents: Pd-Catalyzed 2-Pyridylation Reaction of Aryl Halides
Wei Li1,#, Yu Chen1,#, Ruyi Yuan1, Xuhao Jia1, Yingming Yao1, Li Zhang1 (张力)*
1Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, P. R. China.
Angew. Chem. Int. Ed. 2025, 64, e202500315
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.
Article information: //doi.org/10.1002/anie.202500315
