Chinese Journal of Organic Chemistry ›› 2026, Vol. 46 ›› Issue (3): 951-960.DOI: 10.6023/cjoc202509006 Previous Articles     Next Articles

ARTICLES

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, 沈小倩, 王庆许, 柳忠全*()   

  1. 南京中医药大学药学院 南京 210023
  • 收稿日期:2025-09-05 修回日期:2025-11-18 发布日期:2025-12-25
  • 通讯作者: 柳忠全
  • 基金资助:
    国家自然科学基金(22371129)

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

Xianting Huang, Xiaoqian Shen, Qingxu Wang, Zhongquan Liu*()   

  1. College of pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023
  • Received:2025-09-05 Revised:2025-11-18 Published:2025-12-25
  • Contact: Zhongquan Liu
  • Supported by:
    National Natural Science Foundation of China(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, a green and practical strategy for synthesizing such compounds was reported. 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