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立体控制的 (-) - 埃菲德拉丁A (奥兰丁) 的总合成
Wataru Kurosawa1, Toshiyuki Kan, Tohru Fukuyama
1Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Journal of the American Chemical Society
|July 3, 2003
概括
通过使用新的不对称反应和宏循环构造策略,实现了对 (-) - 埃菲德拉丁A 的立体控制总合成. 这一突破为访问复杂的自然产品提供了新的途径.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 自然产品的合成自然产品的合成
背景情况:
- (-) - - 乙烯A是一种复杂的天然产品,具有潜在的生物活性.
- 有效和立体控制的合成路径对于其进一步的研究和开发至关重要.
研究的目的:
- 为了实现第一次立体控制的 (-) - 埃菲德拉丁A的总合成,A.
- 开发和展示适用于复杂自然产品的新型合成方法.
主要方法:
- 不对称的C-H插入反应.
- 内部分子胺-胺交换反应
- 没有尖的不对称的氨基基化反应.
- 对于宏观循环结构的NS策略和分子内aza-Wittig反应.
主要成果:
- 成功的立体控制总合成 (-) - 埃菲德拉丁A.
- 在复杂的分子环境中展示关键的键键形成反应.
- 宏观循环核心结构的高效构建.
结论:
- 开发的合成策略是有效的获取 (-) - 埃菲德拉丁A.
- 使用的方法为合成相关的自然产品提供了潜力.
- 这种合成为生物评估和结构-活性关系研究开辟了道路.
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