高喜树碱的合成研究进展

Research Progress in the Synthesis of Homocamptothecin

目前文献报道的高喜树碱合成方法主要是半合成和全合成两类,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。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。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。

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. 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. The outlook of homocamptothecin in the field of medicine was foreshown,with the indication of the future research direction.