| 李尚丰,马秀光.化学通报,2018,81(3):203-208. |
| 高喜树碱的合成方法及进展探讨 |
| Synthetic Protocols Introduction and Progress of Homocamptothecin |
| 投稿时间：2017-05-17 修订日期：2017-08-17 |
| DOI： |
| 中文关键词: 高喜树碱, 拓扑抑制酶I |
| 英文关键词:Homocamptothecin, topoisomerase I |
| 基金项目: |
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| 中文摘要: |
| 本文概述了近年来国内外高喜树碱的研究现状，对各个研究小组的研究成果进行了较深入的介绍，并对他们的合成方法做了分类梳理。目前文献报道主要是半合成方法和全合成方法两大类，前者方法简单，便捷，但取代基种类太少，而且扩环后，只能得到消旋的高喜树碱。后者虽然方法复杂，但可以在A环和B环上引入各种需要的取代基，目标分子丰富，并且能进行不对称合成。另外，展望了高喜树碱在医药领域的发展前景，为今后研究指明了发展方向。 |
| 英文摘要: |
| All the study advance of homocamptothecin at home and abroad was reviewed. Each group’s synthetic protocol was introduced in depth along with their research results. To date, there have been two ways to synthesize homocamptothecin including semi-synthesis and total synthesis. The former is simple and concise, yet with few substituent groups. It only produces the racemic homocamptothecin. On the contrary, the latter can introduce various substituent groups on ring A and B. This protocol can bring the asymmetric synthesis into practice, though the route seems a little lengthy. The outlook of homocamptothecin in the field of medicine was foreshown, with the indication of the future research direction. |
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