Metal-free synthesis of 3-trifluoromethyl-1,2,4-triazoles via oxidative cyclization of trifluoroacetimidohydrazides with N,N-dimethylformamide as carbon synthons  

作　　者：Shu-Ning Lu Jiajun Zhang Jingxian Li Zhengkai Chen Xiao Feng Wu 

机构地区：[1]Department of Chemistry,Key Laboratory of Surface&Interface Science of Polymer Materials of Zhejiang Province,Zhejiang Sci-Tech University,Hangzhou 310018,China [2]Dalian National Laboratory for Clean Energy,Dalian Institute of Chemical Physics,Chinese Academy of Sciences,Dalian,116023,China [3]Leibniz-Institut für Katalyse e.V.,Albert-Einstein-Straβe 29a,Rostock 18059,Germany

出　　处：《Green Synthesis and Catalysis》2022年第4期385-388,共4页绿色合成与催化（英文）

基　　金：We thank the financial support from the Natural Science Foundation of Zhejiang Province(No.LY19B020016);the K.C.Wong Education Foundation(No.GJTD-2020-08).

摘　　要：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.

关 键 词：METAL-FREE Oxidative cyclization 3-Trifluoromethyl-1 2 4-triazole Trifluoroacetimidohydrazides N N-DIMETHYLFORMAMIDE Trifluoromethyl-substituted N-Heterocycles 

分 类 号：O62[理学—有机化学]