Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University , Tianjin 300072, China.
J Org Chem. 2014 May 16;79(10):4687-93. doi: 10.1021/jo500298j. Epub 2014 Apr 28.
The biologically important 1,2,4-triazolo[1,5-a]pyridines were readily synthesized from N-(pyridin-2-yl)benzimidamides via phenyliodine bis(trifluoroacetate)-mediated intramolecular annulation. This novel strategy allows for the convenient construction of a 1,2,4-triazolo[1,5-a]pyridine skeleton through direct metal-free oxidative N-N bond formation, featuring a short reaction time and high reaction yields.
生物重要的 1,2,4-三唑并[1,5-a]吡啶可以很容易地从 N-(2-吡啶基)苯并咪唑酰胺通过苯碘双(三氟乙酸酯)介导的分子内环化来合成。这种新策略允许通过直接无金属氧化 N-N 键形成方便地构建 1,2,4-三唑并[1,5-a]吡啶骨架,具有反应时间短和反应收率高的特点。