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<p>Regioselective C-H functionalization reactions have emerged as one of the most efficient strategies for the synthesis and modification of organic molecules. However, nondirected regioselective C-H functionalization reactions remain a significant challenge. In this study, we report a novel tetrahydrophenazine-based ligand that enables regioselective <i>meta</i>- or <i>para</i>-C-H arylation of aromatic compounds, attributed to the enhanced steric effects imparted by its scaffold. This strategy facilitates the late-stage modification of pharmaceutical molecules, offering a new model for nondirected site-selective C-H activation.</p>

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Palladium-catalyzed ligand for sterically enabled nondirected distal-selective C-H arylation of arenes

  • 期刊论文

  • 发表日期：

    2025年6月4日

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  • Xu Xu,
  • Zhiyu Cao,
  • Jingyu Zhang,
  • Yingsheng Zhao

摘要

Regioselective C-H functionalization reactions have emerged as one of the most efficient strategies for the synthesis and modification of organic molecules. However, nondirected regioselective C-H functionalization reactions remain a significant challenge. In this study, we report a novel tetrahydrophenazine-based ligand that enables regioselective meta- or para-C-H arylation of aromatic compounds, attributed to the enhanced steric effects imparted by its scaffold. This strategy facilitates the late-stage modification of pharmaceutical molecules, offering a new model for nondirected site-selective C-H activation.