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综述与进展

具有生物活性的 C2手性-4-色满酮衍生物的不对称合成研究进展

王桂霞, 龚木兰, 杜金龙, 程啟明, 苗力文, 孔翔飞*   

  1. 桂林理工大学化学与生物工程学院 桂林 541004
  • 收稿日期:2026-01-24 修回日期:2026-03-29
  • 基金资助:
    国家自然科学基金地区科学基金项目(22261014).

Progress in the asymmetric synthesis of C2 chiral-4-chromanone derivatives with bioactivities

Wang Guixia, Gong Mulan, Du Jinlong, Cheng Qiming, Miao Liwen, Kong Xiangfei*   

  1. College of Chemistry and Biological Engineering, Guilin University of Technology, Guilin, 541004
  • Received:2026-01-24 Revised:2026-03-29
  • Contact: *E-mail: xiangfei.kong@glut.edu.cn
  • Supported by:
    National Science Foundation of China (Grant Nos. 22261014)

C2手性-4-色满酮因其显著的生物活性而备受关注。有关 C2手性-4-色满酮衍生物的不对称合成已成为有机合成领域的研究热点之一,其中以色烯酮为底物,通过 C2=C3双键的不对称加成得到 C2手性-4-色满酮衍生物,因前体化合物易得、立体选择性强、原子经济性高,成为此类衍生物合成的主要途径之一。本文综述了近十年此类合成方法的研究报道,其中主要介绍了通过金属手性配合物参与的不对称催化。对比分析不同催化体系下立体选择性的反应机理,归纳总结了有利于提高立体选择性的催化体系结构特点,并对此领域当前面临的挑战和未来发展方向进行了展望。

关键词: 生物活性, 色烯酮, 不对称合成, 金属手性配合物, 色满酮

C2 chiral-4-chromanones have attracted considerable attention owing to their pronounced biological activities. The asymmetric synthesis of C2 chiral-4-chromanone derivatives has therefore emerged as an important research topic in the field of organic synthesis. Among the various strategies, asymmetric addition to chromenones via the C2=C3 double bond represents one of the most widely employed approaches for the construction of C2 chiral-4-chromanone derivatives, owing to the ready availability of the substrates, high stereoselectivity, and excellent atom economy. This review summarizes research reports on this type of synthetic methodology over the past decade, with a focus on asymmetric catalysis mediated by chiral metal complexes. It provides a comparative analysis of the stereoselective mechanisms under different catalytic systems, summarizes the structural features of catalytic systems that are beneficial for enhancing stereoselectivity, and discusses the current challenges and future perspectives in this field.

Key words: biological activity, chromenone, asymmetric synthesis, chiral metal complex, chromanones