School of Pharmacy, Yancheng Teachers University, Yancheng 224007, China.
College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, Nanjing 211816, China.
Org Biomol Chem. 2023 May 31;21(21):4440-4444. doi: 10.1039/d3ob00516j.
A green and efficient electrochemical method for the preparation of difluoromethylated indoles has been developed. In this work, sodium difluoromethanesulfinate (HCFSONa) was used as the fluorinating reagent, and various indole derivatives with difluoromethylation at the C-2 position were obtained in moderate to good yields under catalyst- and oxidant-free conditions. Moreover, this C-2 difluoromethylation protocol is operationally simple, proceeds at room temperature, and can be easily scaled up. Cyclic voltammetry (CV) and control experiments indicated that this transformation may proceed a radical pathway.
一种绿色高效的电化学方法被开发用于制备二氟甲基吲哚。在这项工作中，使用二氟甲磺酸钠（HCFSONa）作为氟化试剂，在无催化剂和氧化剂的条件下，各种吲哚衍生物在 C-2 位以中等至良好的产率得到二氟甲基化产物。此外，这种 C-2 二氟甲基化方法操作简单，在室温下进行，并且可以很容易地放大。循环伏安法（CV）和控制实验表明，这种转化可能通过自由基途径进行。
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