Metal-free Synthesis of 5-Trifluoromethyl-1,2,4-triazoles via elemental sulfur promoted oxidative cyclization of trifluoroacetimidohydrazides with benzylic and aliphatic amines,Molecular Catalysis

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Metal-free Synthesis of 5-Trifluoromethyl-1,2,4-triazoles via elemental sulfur promoted oxidative cyclization of trifluoroacetimidohydrazides with benzylic and aliphatic amines
Molecular Catalysis ( IF 3.9 ) Pub Date : 2022-05-01 , DOI: 10.1016/j.mcat.2022.112336
Shu-Ning Lu ₁ , Yue Sun ₁ , Jiajun Zhang ₁ , Zhengkai Chen ₁ , Xiao-Feng Wu _{2,

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Affiliation

An elemental sulfur-mediated oxidative cyclization of readily available trifluoroacetimidohydrazides and aliphatic amines has been achieved, which provided a direct avenue to structurally diverse 5-trifluoromethyl-1,2,4-triazoles. In this transformation, sulfur acts as a traceless oxidizing agent. A myriad of benzyl amines and tertiary aliphatic amines were tolerated in this protocol. The reaction can be scaled up easily and also been applied to build GlyT1 inhibitor as an example of bio-active molecule.

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