聚环分子的融合和立体选择组合的策略
Emily E Robinson1, Regan J Thomson1
1Department of Chemistry, Northwestern University , 2145 Sheridan Road, Evanston, Illinois 60208, United States.
Journal of the American Chemical Society
|January 9, 2018
概括
研究人员开发了一种新的合成方法, 这种强大的策略产生了多样化的结构,在医学上有潜在的应用,包括细胞毒性化合物和抗疟疾药物.
科学领域:
- 有机化学
- 合成化学
- 医学化学
背景情况:
- 多环架是许多具有显著生物活性的自然产品的核心结构.
- 开发高效和模块化合成路径对这些复杂的分子仍然是有机化学的一个关键挑战.
研究的目的:
- 为各种多环架的立体选择性合成建立一个通用和强大的反应序列.
- 展示在生物活性天然产品中发现的基层结构的模块化策略.
- 通过复杂的自然产品的正式合成来展示开发方法的实用性.
主要方法:
- 使用西二醇的刻板选择性氧化合.
- 随后的环闭转化形成多环系统.
- 一种海洋二氧化的 (+) -7,20-二氧化合成.
主要成果:
- 为制备多种多环基支架建立了通用和强大的反应序列.
- 模块化策略成功构建了各种替代和碳循环基结构.
- 一些合成的化合物对瘤细胞系表现出强烈的细胞毒性.
- 实现了 (+) -7,20-二酸的简洁和融合的17步形式合成.
结论:
- 开发的合成策略是访问复杂的多环分子的多功能工具.
- 该方法可制备具有潜在治疗用途的化合物,包括抗癌和抗疟疾活性.
- 这种方法提供了一个模块化和高效的自然产品的基础结构和类型.
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