Jiangsu Key Laboratory for the Research and Utilization of Plant Resources, the Jiangsu Provincial Platform for Conservation and Utilization of Agricultural Germplasm, Institute of Botany, Jiangsu Province and Chinese Academy of Sciences, Nanjing 210014, China.
School of Chemistry and Chemical Engineering, Xuchang University, Henan 461000, China.
J Org Chem. 2022 Nov 4;87(21):14514-14522. doi: 10.1021/acs.joc.2c01926. Epub 2022 Oct 20.
A base-mediated (3 + 2) cycloaddition of trifluoroacetohydrazonoyl chlorides with imidates for the construction of 3-trifluoromethyl-1,2,4-triazoles has been described. This reaction is characterized by readily starting materials, simple reaction conditions, good yields, a broad substrate scope, and excellent regioselectivity. The utility of this protocol has been validated by the synthesis of a drug-like molecule.
三氟乙酰腙酰氯与异氰酸酯的碱介导（3 + 2）环加成反应构建了 3-三氟甲基-1,2,4-三唑。该反应具有原料易得、反应条件简单、产率高、底物范围广、区域选择性好等特点。该方法的实用性已通过合成类似药物分子得到验证。
