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研究论文

碘催化分子内环化2-羟基-吲哚-3-酮类化合物的合成

何雨蒙†a, 周风院†a, 江楠a, 张玉琦a, 王记江a, 马豪杰*,a,b   

  1. (a延安大学化学与化工学院 陕西省化学反应工程重点实验室 延安 716000)
    (b山东协和学院医学院 济南 250109)
  • 收稿日期:2025-10-23 修回日期:2025-11-21
  • 基金资助:
    陕西省自然科学基础研究计划(No. 2025JC-YBQN-129)、陕西省大学生创新创业训练计划(No. S202410719082)、山东省自然科学基金研究项目(No. ZR2025QC95)资助项目.

Iodine-Catalyzed Intramolecular Cyclization for the Synthesis of 2-hydroxy-indolin-3-ones

Yumeng He†a, Fengyuan Zhou†a, Nan Jianga, Yuqi Zhanga, Jijiang Wanga, Haojie Ma*,a,b   

  1. (aShaanxi Key Laboratory of Chemical Reaction Engineering, College of Chemistry and Chemical Engineering, Yan'an University, Yan'an 716000)
    (bMedical College, Shandong Xiehe University, Jinan 250109)
  • Received:2025-10-23 Revised:2025-11-21
  • Contact: *E-mail: mahj@yau.edu.cn
  • About author:†These authors contributed equally to this work.
  • Supported by:
    Project supported by the Natural Science Foundation Research Project of Shaanxi Province (No. 2025JC-YBQN-129), the Shaanxi province College Students’ Innovation and Entrepreneurship Training Program (No. S202410719082), the Natural Science Foundation Research Project of Shandong Province (No. ZR2025QC95).

报道了一种新颖高效的以N-(2-乙酰苯基)吡啶酰胺为原料,通过碘催化分子内环化合成2-羟基吲哚-3-酮类化合物的策略。该方法具有原子经济、无金属参与、操作简单、试剂便宜等优点,为广泛存在于药物、生物活性分子和天然产物中的2-羟基-吲哚-3-酮类衍生物的合成提供了一条实用而有吸引力的路线.

关键词: 碘, 2-羟基-吲哚-3-酮, N-(2-乙酰苯基)吡啶酰胺, 分子内环化, 非金属

A novel and efficient strategy for the synthesis of 2-hydroxy-indolin-3-ones through iodine-catalyzed intramolecular cyclization of N-(2-acetylphenyl)picolinamide has been developed. This protocol features atom economy, metal-free, easy operation with cheap reagents, providing a useful and attractive route for the synthesis of 2-hydroxy-indolin-3-ones, which is widely presented in and pharmaceuticals, biologically active molecules and natural products.

Key words: iodine, 2-hydroxy-indolin-3-ones, N-(2-acetylphenyl)picolinamide, intramolecular cyclization, metal-free