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四氢吡咯衍生物合成氢化吡咯里嗪研究进展
Recent Advances in the Synthesis of Hydrogenated Pyrrolizines from Tetrahydropyrrole Derivatives

DOI: 10.12677/amc.2026.143029, PP. 284-296

Keywords: 四氢吡咯衍生物,氢化吡咯里嗪,分子内环化,分子间环加成,三组分反应
Tetrahydropyrrole Derivatives
, Hydrogenated Pyrrolizine, Intramolecular Cyclization, Intermolecular Cycloaddition, Three-Component Reaction

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Abstract:

吡咯里嗪及其氢化衍生物作为一类重要的含氮稠环骨架,广泛分布于天然生物碱、药物分子及其他生物活性化合物中,在材料科学与有机合成领域展现出重要的研究价值。由于其独特的氮杂双环结构与多样的立体化学特征,发展高效、简便的合成方法始终是该领域的研究重点。本文以四氢吡咯及其衍生物为关键前体,围绕氢化吡咯里嗪骨架的构建策略展开综述。重点阐述了分子内环化、分子间环加成及三组分反应在目标化合物合成中的应用,并对各方法的反应特征及底物适用性进行了归纳总结,以期为氢化吡咯里嗪衍生物的快速构建提供有益参考。
Pyrrolizine and its hydrogenated derivatives constitute an important class of nitrogen-fused heterocycles widely distributed in natural alkaloids, pharmaceuticals, and bioactive compounds, with significant value in materials science and organic synthesis. Their unique diazabicyclic framework and diverse stereochemical features have driven sustained efforts toward developing efficient synthetic methodologies. This review comprehensively summarizes construction strategies for hydrogenated pyrrolizine scaffolds using tetrahydropyrrole and its derivatives as key precursors, with emphasis on intramolecular cyclization, intermolecular cycloaddition, and three-component reactions. The reaction characteristics and substrate scope of each approach are systematically delineated to provide valuable references for the rapid assembly of hydrogenated pyrrolizine derivatives.

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