Department of Chemistry, Vali-e-Asr University, Rafsanjan, 77176, Iran.
Mol Divers. 2020 Nov;24(4):1301-1312. doi: 10.1007/s11030-019-09995-8. Epub 2019 Sep 25.
A fast and convenient method for synthesis of 1,3-diaryl-5-(trifluoromethyl)-1H-1,2,4-triazole compounds has been described via intramolecular oxidative cyclization of the N-(2,2,2-trifluoro-1-(arylimino)ethyl)benzimidamide intermediates by I/KI in excellent yields without any purification. N-(2,2,2-Trifluoro-1-(arylimino)ethyl)benzimidamide intermediates which are used in this project have been synthesized from the reaction of N-aryl-2,2,2-trifluoroacetimidoyl chlorides and benzamide hydrochloride derivatives at room temperature for the first time.
通过 N-(2,2,2-三氟-1-(芳基亚氨基)乙基)苯甲脒中间体的分子内氧化环化,I/KI 在没有任何纯化的情况下以优异的收率高效合成了 1,3-二芳基-5-(三氟甲基)-1H-1,2,4-三唑化合物。本项目中使用的 N-(2,2,2-三氟-1-(芳基亚氨基)乙基)苯甲脒中间体是首次通过 N-芳基-2,2,2-三氟乙酰胺酰氯和苯甲酰胺盐酸盐衍生物在室温下反应合成的。