| 彭碧,曹盼盼,康亮亮,李佳铮,阙妍炎,方引,何述钟.化学通报,2021,84(9):888-894. |
| Thapsigargin的全合成研究进展 |
| Research Progress on Total Synthesis of Thapsigargin |
| 投稿时间：2021-03-03 修订日期：2021-03-26 |
| DOI： |
| 中文关键词: Thapsigargin 全合成 倍半萜内酯 cis-5/7/5稠环体系 |
| 英文关键词:Thapsigargin total synthesis sesquiterpene lactone 5/7/5 tricyclic ring system |
| 基金项目:国家自然科学基金项目(2206010324)资助 |
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| 中文摘要: |
| Thapsigargin是一类从地中海植物毒胡萝卜(thapsia garganica )中分离得到的结构复杂的高氧化态倍半萜内酯,其对肌浆-内质网Ca离子- ATP泵(SERCAs)具有不可逆的抑制作用。鉴于其良好的生物活性而备受有机合成化学家的广泛关注。在合成中,立体选择性地构建该分子cis-5/7/5稠环体系以及多个手性中心是极具挑战性的。本文综述了三个课题组的全合成研究工作, 为该类天然产物的进一步研究提供参考。 |
| 英文摘要: |
| Thapsigargin, which was isolated from the Mediterranean plant Thapsia garganica., is a sesquiterpene lactone with highly oxidized tricyclic core structure. Due to its excellent inhibitory activity against sarco/endoplasmic reticulum Ca2+-ATPases (SERCAs), this molecule has attracted lots attention from pharmaceutical academia. From the synthetic view, the highly functionalized 5/7/5 tricyclic ring system represents a significant challenge. This article reviews all the three total syntheses of thapsigargin till 2020. |
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