Cen Kaili, Wei Jiahao, Feng Yuting, Liu Yuan, Wang Xinye, Liu Yangyu, Yin Yalin, Yu Junhong, Wang Dahan, Cai Jinhui
College of Chemistry and Chemical Engineering, University of South China, Hengyang 421001, Hunan, China.
School of Pharmaceutical Science, University of South China, Hengyang 421001, Hunan, China.
Org Biomol Chem. 2023 Sep 13;21(35):7095-7099. doi: 10.1039/d3ob01133j.
Here we report a strategy for the facile assembly of fused 3-trifluoromethyl-1,2,4-triazoles, which are difficult to synthesize using traditional strategies, in 50-96% yields through a triethylamine-promoted intermolecular [3 + 2] cycloaddition pathway. This protocol features high efficiency, good functional group tolerance, mild conditions, and easy operation. Furthermore, a gram-scale reaction and product derivatizations were carried out smoothly to illustrate the practicability of this method.
在此，我们报道了一种简便合成稠合3-三氟甲基-1,2,4-三唑的策略，这类化合物用传统方法难以合成，通过三乙胺促进的分子间[3 + 2]环加成途径，产率为50 - 96%。该方法具有高效、良好的官能团耐受性、温和的条件及操作简便等特点。此外，顺利进行了克级规模反应及产物衍生化，以说明该方法的实用性。
