分子内苯并呋喃衍生物合成研究进展
Research Progress on the Synthesis of Intramolecular Benzofuran Derivatives
摘要: 苯并呋喃是众多天然产物和药物分子的核心结构骨架，其高效、绿色的合成策略一直是有机合成领域的研究重点。分子内环化是构建此类杂环的高效方法，其路径可根据形成的关键化学键分为四种经典类型：O-C2键的形成(如邻炔基酚的羟烷氧基化)、Cβ-O键的形成(如邻卤苯乙炔的环化)、C2-C3键的形成(如分子内aldol缩合)以及C3-Cα键的形成(如Friedel-Crafts酰基化)。传统方法常依赖化学计量的氧化剂或强酸/碱，而近年来，随着绿色化学理念的深入，该领域涌现出许多创新技术，如过渡金属催化的C-H活化、无氧化剂环化以及光促进反应等。这些进展显著提升了合成的原子经济性和步骤效率，为复杂苯并呋喃衍生物的合成提供了更为精准和可持续的解决方案。
Abstract: Benzofuran is the core structural skeleton of many natural products and drug molecules, and its efficient and green synthesis strategy has always been a research focus in the field of organic synthesis. Intramolecular cyclization is an efficient method for constructing such heterocycles, and its pathways can be classified into four classic types based on the key chemical bonds formed: O-C2 bond formation (such as hydroxyalkoxylation of ortho alkynyl phenols), Cβ-O bond formation (such as cyclization of ortho halogenated phenylacetylene), C2-C3 bond formation (such as intramolecular aldol condensation), and C3-Cα bond formation (such as Friedel Crafts acylation). Traditional methods often rely on stoichiometric oxidants or strong acids/bases, but in recent years, with the deepening of green chemistry concepts, many innovative technologies have emerged in this field, such as transition metal catalyzed C-H activation, oxidant free cyclization, and photo promoted reactions. These advances have significantly improved the atomic economy and step efficiency of synthesis, providing more precise and sustainable solutions for the synthesis of complex benzofuran derivatives.
文章引用：吉江涛, 张轩. 分子内苯并呋喃衍生物合成研究进展[J]. 有机化学研究, 2025, 13(4): 335-347. https://doi.org/10.12677/jocr.2025.134033

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