南京大学谢劲团队报道了N-杂芳烃的光诱导无金属/添加剂二氟甲基化。相关研究成果于2025年1月16日发表于国际一流学术期刊《中国化学》。

该文中，研究人员报告了一种光诱导、无金属/添加剂的策略，用[双(二氟乙酰氧基)碘]苯作为二氟甲基化试剂，对N-杂芳族化合物进行双氟甲基化。

该方案以中等至良好的收率（高达91%）制备二氟甲基化N-杂芳族化合物。该转化与多种底物相容，对各种官能团具有良好的耐受性。

此外，该方法在克级合成和生物重要分子后期功能化中的应用，进一步证明了其合成价值。

附：英文原文

Title: Photoinduced Metal-/Additive-Free Difluoromethylation of N-Heteroaromatics†

Author: Congjun Zhu, Yangyang Shen, Tao Guo, Qing Yang, Dongpu Zhao, Huiqing Yang, Jin Xie

Issue&Volume: 2025-01-16

Abstract: Herein, we report a photo-induced, metal-/additive-free protocol for the difluoromethylation of N-heteroaromatics with [bis(difluoroacetoxy)iodo]benzene as the difluoromethylation reagent. The protocol affords difluoromethylated N-heteroaromatics in moderate to good yield (up to 91%). The transformation is compatible with a wide range of substrates and has good tolerance towards various functional groups. Moreover, the synthetic value of this method is further demonstrated by applications in gram-scale synthesis and the late-stage functionalization of biologically important molecules.

DOI: 10.1002/cjoc.202401153

Source: https://onlinelibrary.wiley.com/doi/full/10.1002/cjoc.202401153