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无催化剂及无溶剂光引发下氮杂芳烃的自由基脱羧酰基化反应

黄涎廷a, 沈小倩a, 王庆许a, 柳哲怀b, 黄也b, 柳忠全*,a   

  1. a南京中医药大学 江苏 南京 210023;
    a句容碧桂园学校 江苏 镇江 212446
  • 收稿日期:2025-09-05 修回日期:2025-11-18
  • 基金资助:
    国家自然科学基金(No. 22371129)资助项目.

A Catalyst and Solvent-Free Photochemical Acylation of N-Heteroarenes with Keto Acids

Xianting Huanga, Xiaoqian Shena, Qingxu Wanga, Zhehuai Liub, Ye Huangb, Zhong-Quan Liu*,a   

  1. aNanjing University of Chinese Medicine, Nanjing 210023;
    bJurong Country Garden School, Zhenjiang 212446
  • Received:2025-09-05 Revised:2025-11-18
  • Contact: *E-mail: liuzhq@lzu.edu.cn
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 22371129).

The N-heteroaryl ketones are an important class of synthetic intermediates, and their skeletal structures are widely found in natural products, drug molecules, and materials. Acylation of N-heterocycles by keto acid decarboxylation is an effective strategy for constructing N-heteroaryl ketone compounds. However, the reported synthesis methods generally require transition-metal catalysts, a large amount of chemical oxidants, photosensitizers, etc., which limits their industrial applications. Herein, we report a green and practical strategy for synthesizing such compounds. Blue light irradiation of the mixture of N-heteroaromatics and α-ketoacids can lead to high-yield, high selectivity, and large-scale synthesis of the corresponding acylated N-heteroarenes. This system does not require any photosensitizers, catalysts, oxidants, or solvents. In addition, it is worth noting that this system does not even require continuous blue light irradiation, only light triggering is sufficient to promote this process.

Key words: Free-radical chemistry, Photochemistry, Decarboxylation, Acylation, N-Heteroarenes, Solvent-free