Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 21, Issue 35, Pages 7095-7099Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d3ob01133j
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This study presents a strategy for the efficient synthesis of fused 3-trifluoromethyl-1,2,4-triazoles using a triethylamine-promoted intermolecular [3 + 2] cycloaddition pathway. The method exhibits high efficiency, good functional group tolerance, mild conditions, and ease of operation. Additionally, gram-scale reactions and product derivatizations were successfully conducted, demonstrating the practicality of this approach.
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.
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