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尿嘧啶及其衍生物的C-H官能化反应研究进展

胡甜芯, 陈斌斌, 王泽艺, 陈漫仪, 章鹏飞, 徐骏*   

  1. 杭州师范大学材料与化学化工学院 有机硅化学及材料技术教育部重点实验室 全省有机硅材料技术重点实验室 浙江 杭州 311121
  • 投稿日期:2026-04-27
  • 作者简介:胡甜芯,杭州师范大学材料化学与化工学院2024级本科生, 研究方向为绿色有机合成方法学研究.陈斌斌,杭州师范大学材料与化学化工学院2023级研究生, 研究方向为电化学有机合成.王泽艺,杭州师范大学材料与化学化工学院2024级研究生, 研究方向为光催化有机合成.陈漫仪,杭州师范大学材料与化学化工学院2024级研究生, 研究方向为光催化有机合成.章鹏飞,杭州师范大学材料与化学化工学院教授、博士生导师,英国皇家化学会会士,享受国务院政府特殊津贴专家,浙江省“万人计划”杰出人才。主要从事氟/硅精细化学品创制、碳氢键催化活化及光催化自由基偶联研究。 徐骏,杭州师范大学材料与化学化工学院讲师、硕士生导师,主要从事绿色有机合成方法学及精细化学品新工艺研发,相关成果发表于ACS Catal.、Green Chem.、Adv. Funct. Mater.、Chin. Chem. Lett.、Org. Lett.等期刊;现担任Chin. Chem. Lett.、Chin. J. Org. Chem.等期刊的青年编委。
  • 基金资助:
    浙江省自然科学基金(LQN26B060020)杭州市自然科学基金(No. 2025SZRJJ0081)国家自然科学基金 (No. 22508079)资助项目.

Research Progress on C-H Functionalization Reactions of Uracil and Its Derivatives

Hu Tianxin, Chen Binbin, Wang Zeyi, Chen Manyi, Zhang Pengfei, Xu Jun*   

  1. College of Material, Chemistry and Chemical Engineering, Key Laboratory of Organosilicon Chemistry and Material Technology, Ministry of Education, Zhejiang Key Laboratory of Organosilicon Material Technology, Hangzhou Normal University, Hangzhou, 311121, China
  • Received:2026-04-27
  • Contact: * E-mail: xujunchem@hznu.edu.cn.
  • Supported by:
    Zhejiang Provincial Natural Science Foundation of China (LQN26B060020), the Natural Science Foundation of Hangzhou City (No. 2025SZRJJ0081), and the National Natural Science Foundation of China (No. 22508079).

尿嘧啶及其衍生物是生物医药、生命科学与农业科学领域的核心骨架分子,其结构修饰具有重要的研究与应用价值。传统修饰方法如缩合环化、亲核取代等多依赖高温、强酸或强碱等苛刻条件,存在位点选择性差、原子经济性低、底物适用范围窄及环境不友好等问题,难以满足现代药物后期修饰与工业化生产的需求。近年来,直接C-H官能化反应凭借其无需预官能团化、步骤经济性高、原子经济性好等优势,为尿嘧啶类化合物的高效、绿色修饰提供了新策略。本文系统综述了近六年来尿嘧啶及其衍生物C-H官能化的研究进展,涵盖烷基化、芳基化、三氟甲基化、酰化、胺化、硫/硒化、硅化、烯基化及硼化等多种转化类型。文章围绕底物适用范围、反应机理及应用潜力进行深入比较,并结合本课题组相关工作,旨在为相关领域的研究者提供系统参考,推动尿嘧啶类分子在药物研发与生命科学中的创新应用。

关键词: 尿嘧啶, C-H官能化反应, 自由基, 光催化, 偶联反应

Uracil and its derivatives are core structural motifs in the fields of biomedicine, life sciences, and agricultural sciences, and their structural modification holds significant research and application value. Traditional modification methods, such as condensation cyclization and nucleophilic substitution, often rely on harsh conditions including high temperatures, strong acids, or strong bases. These approaches suffer from poor site selectivity, low atom economy, narrow substrate scopes, and environmental unfriendliness, failing to meet the demands of modern late-stage drug modification and industrial production. In recent years, direct C-H functionalization has emerged as a novel strategy for the efficient and green modification of uracil compounds, leveraging advantages such as the avoidance of pre-functionalization, high step economy, and excellent atom economy. This review systematically summarizes the progress in C-H functionalization of uracil and its derivatives over the past six years, covering various transformation types including alkylation, arylation, trifluoromethylation, acylation, amination, sulfidation/selenization, silicidation, alkenylation, and boronation. This article provides an in-depth comparison of substrate scopes, reaction mechanisms, and application potentials. By also incorporating relevant work from our research group, we aim to offer researchers in related fields a systematic and detailed reference framework to facilitate innovative applications of uracil-based molecules in drug discovery and life sciences.

Key words: uracil, C-H functionalization, radical, photocatalysis, coupling reaction