Malagasy生物碱的合成研究进展
收稿日期: 2024-07-18
修回日期: 2024-09-25
网络出版日期: 2024-11-08
基金资助
江苏省自然科学基金(BK20210939); 国家自然科学基金(22401019)
Recent Progress in the Synthesis of the Malagasy Alkaloids
Received date: 2024-07-18
Revised date: 2024-09-25
Online published: 2024-11-08
Supported by
Natural Science Foundation of Jiangsu Province(BK20210939); National Natural Science Foundation of China(22401019)
Malagasy生物碱具有特征的反式稠合C/D环系以及多个连续手性中心, 为其合成研究带来了巨大挑战. 此类生物碱还具有潜在的抗疟增效活性, 尤其是malagashanine作为天然增敏剂, 可以提升耐药疟原虫对于氯喹的敏感性. 独特而极具挑战性的结构以及明确的药理活性, 使得此类天然产物的合成研究颇具吸引力, 同时对于新型抗疟药物的研发也具有重要价值. 本综述总结了目前Malagasy生物碱的合成研究进展, 包括半合成研究、核心骨架构建以及全合成研究.
关键词: Malagasy生物碱; 全合成; 骨架构建; 半合成; 抗疟活性
何卫刚 , 刘亚东 , 邓迎开 , 孙先宇 . Malagasy生物碱的合成研究进展[J]. 有机化学, 2025 , 45(4) : 1153 -1165 . DOI: 10.6023/cjoc202407032
The Malagasy alkaloids have characteristic trans-fused C/D ring systems and multiple chiral centers, which pose great challenge for their synthesis research. These alkaloids also have potential synergistic anti-malarial activity, especially malagashanine as a natural sensitizer, which can enhance the sensitivity of drug-resistant plasmodium to chloroquine. The unique and challenging structure combined with preonunced pharmacological activity makes the synthesis of these natural products attractive, and their synthesis research also has important value for the development of new antimalarial drugs. The current research progress in the synthesis of the Malagasy alkaloidshis is summarized, including semi-synthesis, core skeleton construction, and total synthesis.
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