类的总合成 帕林因A和帕林因D
Fang-Xin Wang1, Ji-Yuan Du1, Hui-Bin Wang1
1State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University , 222 Tianshui Nanlu, Lanzhou 730000, China.
Journal of the American Chemical Society
|March 3, 2017
概括
研究人员首次完成了Lycopodium类素palhinine A和D的总合成,这涉及创造一种新的六环前体和一个关键的循环添加物,以构建复杂的异二框架.
科学领域:
- 有机化学
- 自然产品合成
- 医学化学
背景情况:
- 类是一种具有显著生物活性的复杂自然产品.
- 之前的合成努力在构建这些化合物的复杂多环框架方面遇到了挑战.
研究的目的:
- 为了实现第一个全合成Lycopodium甲基帕林因A,帕林因D,以及它们的C3.
- 开发一种新型的合成策略,用于获取高张力多环天然产品.
主要方法:
- 使用连接转换产生六环异素前体.
- 采用微波辅助,区域和立体选择性分子内烯循环添加,形成10-oxa-1-azabicyclo[5.2.1]decane核心.
- 执行了N-O键裂变以构建九个成员的阿佐环.
- 进行了晚期化疗和立体选择性降解β-二甲.
主要成果:
- 已经成功合成了帕林因A,帕林因D和它们的C3体.
- 通过氧桥接器演示了高度紧张的中型环的构造.
- 建立了一个融合合成路径复杂的Lycopodium化物.
结论:
- 开发的合成策略提供了有效的Palhinine A,D和相关类型.
- 这项研究强调了分子内基循环添加在构建复杂的多环系统中的有用性.
- 这项工作扩大了天然产品合成和药物化学探索的合成工具箱.
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