One-step synthesis of cyanated pyrazolo[1,5-a]pyridines utilizing N-aminopyridines as a 1,3-dipole and a nitrogen source

作者：Shi, Xiaotian; Lin, Yu; Wei, Jiaohang; Zhao, Limin; Guo, Pengfeng; Cao, Hua^*; Liu, Xiang^*

来源：Organic Chemistry Frontiers, 2023, 10(12): 2892-2897.

DOI：10.1039/d3qo00417a

• IMINOPYRIDINIUM YLIDES
• RECEPTOR ANTAGONISTS
• POTENT
• CYCLOADDITION
• DERIVATIVES
• DISCOVERY
• CYCLIZATION
• INHIBITORS
• EFFICIENT
• DESIGN

By utilizing the dual reactivity function of N-aminopyridinium ylides, we developed a direct [3 + 2]-cycloaddition of N-aminopyridinium ylides and ynals to build the pyrazolo[1, 5-a]pyridine core while introducing a cyano group. In the transformation, N-aminopyridinium ylide serves as a 1,3-dipole and a nitrogen source, which results in the production of cyanated pyrazolo[1,5-a]pyridines and pyrazolo[1,5-a]pyrazines with a wide scope.

• 单位
  广东药学院