对 (-) - 脑素B的酶选择性总合成
Zezhong Sun1, Shuang Jin1, Jianing Song1
1Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of the Ministry of Education, College of Chemistry & Materials Science, Northwest University, 710127, Xi'an, China.
Angewandte Chemie (International ed. in English)
|October 11, 2023
概括
研究人员首次实现了复杂的天然产品 (-) - 头氨酸B的全合成. 关键的转换包括不对称的迈克尔加法和一种新的Pauson-Khand/deacyloxylation过程.
科学领域:
- 有机化学 有机化学
- 自然产品的合成自然产品的合成
- 药用化学 医学化学
背景情况:
- 塞法洛塔克斯 (Cephalotaxus diterpenoids) 是天然产物,以其独特的结构和生物活动而闻名.
- (-) - - 头素B是一个特别复杂的成员,具有拥挤的七环骨架,三个乳环和九个连续的立体中心.
研究的目的:
- 为了实现第一个enantioselective的 (-) - cephalotanin B.的总合成.
- 开发新的合成方法来构建复杂的多环自然产品.
主要方法:
- 采用了一个不同的不对称的迈克尔加法反应.
- 作为第二代立体选择性Pauson-Khand反应协议的一部分,开发了一种新的Pauson-Khand/deacyloxylation过程.
- 一个环氧化物开放/消除/双乳化级联被用来构建A-B-C环系统.
主要成果:
- 首次对 (-) - - 脑素B的全合成成功完成.
- 展示了新的合成策略和转换,包括一个新的Pauson-Khand/deacyloxylation序列.
- 具有挑战性的螺旋形的A-B-C环系统被高效地构建.
结论:
- 开发的合成途径提供了对 (-) - 脑素B的获取,并展示了创新的化学转化.
- 这种综合验证了新方法在构建复杂分子架构方面的实用性.
- 该研究为天然产品合成和药物化学探索领域做出了贡献.
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