塞拉斯特罗尔的总合成,开发一个平台来获取塞拉斯特罗尔天然产品
Andrew M Camelio1, Trevor C Johnson1,2, Dionicio Siegel1,2
1Chemistry Department, The University of Texas at Austin , Norman Hackerman Building, Austin, Texas 78701, United States.
Journal of the American Chemical Society
|September 3, 2015
概括
研究人员首次合成了包括在内的类天然产品. 这一突破为临床研究中的三烯及其衍生物提供了新的途径.
科学领域:
- 有机化学
- 自然产品合成
- 医学化学
背景情况:
- 类天然产品是一种三烯,正在临床应用中进行研究.
- 这些复杂分子的合成带来了重大挑战.
研究的目的:
- 报告第一个 celastroid 核心结构的化学合成.
- 建立一个合成的途径, 以至于 celastrol 和相关化合物.
主要方法:
- 通过12个步骤的合成,从2,3-二甲基二烯生成了三烯循环化前体.
- 由铁介导的非仿生聚循环形成了五环芯.
- 实现了全碳四元中心的立体特异形成.
主要成果:
- 已经成功合成了一般的化物五环核.
- 进入核心可以制备威尔福酸和威尔福醇A.
- 这些中间体处于赛拉素的途径上.
结论:
- 这项研究介绍了第一个化学合成的 celastroid 核心.
- 开发的合成策略为进一步的研究和开发提供了重要的天然产品.
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