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<p>The incorporation of CF<sub>3</sub> groups into molecules represents a significant strategy in medicinal chemistry, as this modification can profoundly enhance their biological activities. CF<sub>3</sub>-imidoyl sulfoxonium ylides (TFISYs) have emerged as versatile and stable carbene precursors, demonstrating remarkable utility as CF<sub>3</sub>-containing coupling partners for the assembly of diverse CF<sub>3</sub>-heterocycles. This review systematically summarizes recent advances in transition metal-catalyzed, directing group-assisted C–H bond activation reactions employing TFISYs as key coupling partners. The discussion is organized to provide a clear methodological classification based on the multifunctional roles of TFISYs, which can act as alkenylating reagents as well as C1, C2, and C2N1 cyclic unit. A comprehensive evaluation of substrate compatibility, reaction mechanisms, structure modification, and practical applications in functional molecule synthesis is presented.</p> Graphical Abstract <p></p>

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Recent progress in the application of CF3-imidoyl sulfoxonium ylides in transition metal-catalyzed C–H functionalization

  • 期刊论文

  • 发表日期：

    2026年6月19日

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  • Xiaoying Zhao,
  • Dulin Kong,
  • Hongliang Wu,
  • Ruirui Zhai,
  • Xun Chen

摘要

The incorporation of CF3 groups into molecules represents a significant strategy in medicinal chemistry, as this modification can profoundly enhance their biological activities. CF3-imidoyl sulfoxonium ylides (TFISYs) have emerged as versatile and stable carbene precursors, demonstrating remarkable utility as CF3-containing coupling partners for the assembly of diverse CF3-heterocycles. This review systematically summarizes recent advances in transition metal-catalyzed, directing group-assisted C–H bond activation reactions employing TFISYs as key coupling partners. The discussion is organized to provide a clear methodological classification based on the multifunctional roles of TFISYs, which can act as alkenylating reagents as well as C1, C2, and C2N1 cyclic unit. A comprehensive evaluation of substrate compatibility, reaction mechanisms, structure modification, and practical applications in functional molecule synthesis is presented.

Graphical Abstract