The trifluoromethyl group (-CF) containing motifs are valuable leads for the small molecule drug discovery process and have multiple applications in medicine, agriculture, and material science. Not many CF-containing motifs are commercially accessible; therefore, it is critical to design more advanced building blocks. In this work, we demonstrate an oxidant-free, scalable, and user-friendly protocol for the direct C(sp)-H trifluoromethylation of functionalized arenes using Iron(II) triflate as a robust photocatalyst and bench-stable CFSONa (1.5 equiv.) as a CF source under blue light irradiation. This method was extrapolated to >30 examples and compatible with potential functional groups (-NO, -NH, OH, -CHO, -COH, halogens, etc.). Notably, the utility of this approach is showcased for the synthesis of novel CF-containing synthetic building blocks and a few bioactive compounds.

中文翻译：

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三氟甲磺酸铁 (II) 作为光催化剂，在蓝色 LED 灯下进行功能化芳烃的三氟甲基化：获取生物活性化合物


含有三氟甲基（-CF）的基序是小分子药物发现过程的宝贵先导，在医学、农业和材料科学中具有多种应用。商业上可获得的含 CF 基序并不多；因此，设计更先进的构建模块至关重要。在这项工作中，我们展示了一种无氧化剂、可扩展且用户友好的方案，使用三氟甲磺酸铁（II）作为强大的光催化剂和工作台稳定的 CFSONa（1.5 当量）对官能化芳烃进行直接 C(sp)-H 三氟甲基化。 ）作为蓝光照射下的CF光源。该方法被外推到超过 30 个示例，并且与潜在的官能团（-NO、-NH、OH、-CHO、-COH、卤素等）兼容。值得注意的是，该方法在合成新型含 CF 的合成结构单元和一些生物活性化合物方面的实用性得到了展示。