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PhI(OCOCF3)2-Mediated Intramolecular Oxidative N-N Bond Formation: Metal-Free Synthesis of 1,2,4-Triazolo[1,5-a]pyridines

Zisheng Zheng, Shuangyu Ma, Linlin Tang, Daisy Zhang-Negrerie, Yunfei Du* and Kang Zhao*

*Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China, Email:,

Z. Zheng, S. Ma, L. Tang, D. Zhang-Negrerie, Y. Du, K. Zhao, J. Org. Chem., 2014, 79, 4687-4693.

DOI: 10.1021/jo500298j


The biologically important 1,2,4-triazolo[1,5-a]pyridines were readily synthesized from N-(pyridin-2-yl)benzimidamides via PIFA-mediated intramolecular annulation via a direct metal-free oxidative N-N bond formation in short reaction times and high yields.

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Key Words

1,2,4-triazolo[1,5-a]pyridines, PIFA

ID: J42-Y2014