摘要/Abstract

含氮杂环结构广泛存在于天然产物及药物分子中, 具有广谱的生物和药理活性, 受到有机化学家及药物化学家们的高度关注. 开发其绿色、高效的合成方法, 尤其是不对称合成方法一直是热门研究课题. 近年来, 基于脯氨酸等氨基酸手性模块设计合成的系列有机小分子催化剂不断被报道, 为不对称构建含氮杂环化合物提供了高效快捷的途径. 综述了我们研究小组在有机催化不对称构建含氮杂环化合物领域的研究成果, 讨论了关键反应涉及的催化机理.
关键词: 有机催化, 不对称合成, 含氮杂环, 脯氨酸, 焦谷氨酸
Nitrogen-containing heterocyclic structures are widely encountered in natural products and pharmaceuticals, which demonstrate broad-spectrum biological and pharmacological activities, and have attracted intensive attention from organic chemists and medicinal chemists. As a consequence, developing their green and efficient pathways, especially in asymmetric fashion, has always been a hot research field in the synthetic chemistry. In recent years, a series of organocatalysts based on amino acid such as proline and pyroglutamic acid have been reported, which have been well applied in the asymmetric construction of various nitrogen-containing compounds. This account mainly focuses on the research of asymmetric synthesis of nitrogen-containing heterocyclic compounds in our group, and the possible mechanisms of some typical reactions are thus discussed.
Key words: organocatalysis, asymmetric synthesis, N-heterocycle, proline, pyroglutamic acid


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