生物启发的骨多样性类化合物的总合成
Yu-Fei Ou1,2, Yuan Jin1,2, Zai-Feng Yuan1
1State Key Laboratory of Phytochemistry and Natural Medicines, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
研究人员合成了12种Lycopodium类化合物,包括 (-) - 素A,使用一种新的素衍生中间体. 这一突破使得各种各样的化合物结构能够有效地进行不对称的总合成.
科学领域:
- 有机化学
- 自然产品合成
- 医学化学
背景情况:
- 肌骨是Lycopodium类化合物的关键生物遗传中间体.
- 由于其复杂的结构和生物活动,开发高效的合成路径至关重要.
研究的目的:
- 设计和合成一种常见的菌素衍生中间体,用于集体,不对称的Lycopodium类化合物的总合成.
- 首次实现 (-) - 素A的不对称总合成并探索其生物活性.
主要方法:
- 一种由素衍生的常见中间体的设计.
- 从 (R) -pulegone中产的八步合成,具有立体选择的迈克尔添加.
- 选择性碳-碳键形成和骨重组以获取多种类型的基结构.
主要成果:
- 成功合成了五个不同的碳骨架的12个Lycopodium化物.
- 在十度尺度上准备关键中间体.
- 第一个非对称的全合成 (-) - 素A,一个五环化合物.
结论:
- 开发的中间体对于广泛的Lycopodium类化合物的高效,集体和不对称合成至关重要.
- (-) - Hupserrine A具有5-HT3A受体抑制活性 (IC50 = 10. 6μM),这表明其具有潜在的治疗用途.
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