A metal-free approach for the synthesis of 3-trifluoromethyl-1,2,4-triazoles via I₂-mediated oxidative cyclization of readily accessible trifluoroacetimidohydrazides with N,N-dimethylformamide (DMF) has been disclosed. In this transformation, the commonly used organic solvent DMF is applied as a C1 synthon and the methine unit of the 1,2,4-triazole products is independently from N-methyl and N-acyl of DMF. The application potential of the developed method has been demonstrated by the synthesis of the key skeleton of factor IXa inhibitors.

中文翻译：

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以N,N-二甲基甲酰胺为碳合成子的三氟乙酰亚胺基酰肼氧化环化无金属合成3-三氟甲基-1,2,4-三唑

已经公开了一种通过I ₂介导的容易获得的三氟乙酰亚胺基酰肼与N,N -二甲基甲酰胺 (DMF) 的氧化环化来合成 3-三氟甲基-1,2,4-三唑的无金属方法。在该转化中，常用的有机溶剂DMF用作C1合成子，1,2,4-三唑产物的次甲基单元独立于DMF的N-甲基和N-酰基。所开发方法的应用潜力已通过因子 IXa 抑制剂关键骨架的合成得到证明。