While several methods are available for the synthesis of a host of trifluoromethylated heterocycles, very few of them have been applied to access 4-trifluoromethylated 1,2,3-triazoles. We report herein a general methodology for the trifluoromethylation of 1-aryl-4-iodo-1, 2, 3-triazoles. Tetrabutylammonium iodide (TBAI) has been shown to provide enhanced conversion in these CuI-mediated reaction using methyl 2,2-difluoro-2-(fluorosulfonyl)acetate (MDFA). The method exhibited broad functional group tolerance and was applied to the synthesis of a library of 1-aryl-4-trifluoromethyl-1,2,3-triazoles on the multi-gram scale.

中文翻译：

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甲基-2,2-二氟-2-（氟磺酰基）乙酸甲酯（MDFA）/碘化铜（I）和碘化四丁基铵促进1-芳基-4-碘-1,2,3-三唑的三氟甲基化

尽管有几种方法可用于合成大量的三氟甲基化杂环，但很少有方法可用于合成4-三氟甲基化的1,2,3-三唑。我们在此报告了1-芳基-4-碘-1、2、3-三唑的三氟甲基化的一般方法。在使用2，2-二氟-2-（氟磺酰基）乙酸甲酯（MDFA）的CuI介导的反应中，碘化四丁基铵（TBAI）已显示出增强的转化率。该方法表现出宽泛的官能团耐受性，并被用于以克为单位合成1-芳基-4-三氟甲基-1,2,3-三唑的文库。