有机化学    

综述与进展

三氟甲氧基化反应研究进展

马占彩a, 汤平平*,a   

  1. a南开大学化学学院 元素有机化学全国重点实验室 天津 300071
  • 收稿日期:2026-04-23 修回日期:2026-05-25

Advances in Trifluoromethoxylation Reactions

Ma Zhancaia, Tang Pingping*,a   

  1. aState Key Laboratory and Institute of Elemento-Organic Chemistry, Frontiers Science Center for New Organic Matter, College of Chemistry, Nankai University, Tianjin, 300071
  • Received:2026-04-23 Revised:2026-05-25
  • Contact: *E-mail: ptang@nankai.edu.cn
  • Supported by:
    National Key Research and Development Program of China (No. 2025YFA151110), the NFSC (21925105 and 92156001), Fundamental and Interdisciplinary Disciplines Breakthrough Plan of the Ministry of Education of China (JYB2025XDXM410), the Natural Science Foundation of Tianjin (grant no. 24JCZDJC00700, 25ZXZSSS00720).

氟化及含氟官能团化有机化合物在制药、农用化学品及材料科学领域的重要性日益凸显. 其中, 三氟甲氧基(OCF₃)结构单元因其良好的代谢稳定性、适中的亲脂性以及独特的电子效应备受青睐并得到广泛应用. 近年来, 一系列创新性合成策略已被成功开发用于构建含OCF₃的有机分子. 本研究小组长期致力于三氟甲氧基化试剂与方法的研究.本专题重点论述了2021-2026年间我们研究小组在三氟甲氧基化反应领域取得的研究成果, 并重点评述了这些方法在功能分子构建中的应用.

关键词: 三氟甲氧基, 苯磺酸三氟甲酯 (TFMS), N-OCF3双功能试剂

Fluorinated organic compounds are playing an increasingly vital role in pharmaceuticals, agrochemicals, and materials science. With superior metabolic stability, moderate lipophilicity, and unique electronic effects, the trifluoromethoxy (OCF₃) group is a highly valued structural motif. In recent years, a variety of innovative synthetic strategies have been developed for the efficient construction of OCF₃-containing organic molecules. Our research group has long been dedicated to the development of novel trifluoromethoxylation reagents and methodologies. This review summarizes our recent progress in the field of trifluoromethoxylation reactions achieved between 2021 and 2026, with a particular focus on the application of these methods in the synthesis of functional molecules.

Key words: Trifluoromethoxylation, Trifluoromethyl aryl sulfonate (TFMS), Bifunctional N-OCF3 reagent