Metal-free synthesis of 3-trifluoromethyl-1,2,4-triazoles via multi-component reaction of trifluoroacetimidoyl chlorides, hydrazine hydrate and benzene-1,3,5-triyl triformate

Autor: Binjie Wang, Yue Sun, An Cheng, Yeanlun Zhu, Jiye Wang, Zhengkai Chen, Xiao-Feng Wu
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Frontiers in Chemistry, Vol 10 (2022)
Druh dokumentu: article
ISSN: 2296-2646
DOI: 10.3389/fchem.2022.1013977
Popis: A convenient approach for the construction of pharmaceutically valuable 3-trifluoromethyl-1,2,4-triazoles has been developed, which employs the readily available trifluoroacetimidoyl chlorides, hydrazine hydrate and benzene-1,3,5-triyl triformate (TFBen) as starting materials. The multi-component reaction features broad substrate scope, high efficiency, and scalability, providing a facile and straightforward route to the biologically important 3-trifluoromethyl-1,2,4-triazole scaffolds in moderate to good yields. Considering its broad-spectrum pharmaceutical activity, the method offers the opportunity for the further study towards the toxicity risk assessment and structure-activity relationship of the pharmaceuticals containing trifluoromethyl-1,2,4-triazole cores.
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