摘要/Abstract

2-喹啉酮结构单元广泛存在于天然产物和药物活性分子中, 并且是重要的杂环合成砌块. 建立了一种乙酸酐促进下, 环状β-烯胺酮和丙二酸通过[3+3]环合反应构建2-喹啉酮化合物的新方法, 产率为70%~87%. 该方法具有原料简单易得、操作简便、路线简洁、目标化合物可修饰性强等优点.
关键词: β-烯胺酮, 2-喹啉酮, [3+3]环合, 乙酸酐促进
2-Quinolinone unit is frequently found in both natural products and pharmaceuticals. Furthermore, they are important heterocycle building blocks. Herein, a novel approach to the synthesis of 2-quinolinone derivatives has been established from [3+3] cyclization of β-enaminones with malonic acid promoted by acetic anhydride with yields of 70%~87%. The reaction is particularly attractive due to following advantages: simple starting materials, operational simplicity, concise synthetic route, easy purification, highly modifiability of target molecules and so on.
Key words: Keywords β-enaminones, 2-quinolinones, [3+3] cyclization, acetic anhydride promoted


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