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广南素A酒精的总合成

Kenzo Yahata¹, Alois Fürstner¹

¹Max-Planck-Institut für Kohlenforschung, 45470, Mülheim/Ruhr, Germany.

Angewandte Chemie (International ed. in English)

|January 16, 2024

概括

研究人员报告说,他们首次合成了关南氨酸A,这是一个压缩的巨乳. 总合成利用了催化宏循环和催化异构化,实现了酒精前体的良好产量.

科学领域:

有机化学有机化学
药用化学医学化学

背景情况:

广南氨酸A是一种新型的利纳氨酸原体,是一种抗瘤药物.
广南氨酸A具有高度紧张的麦克罗拉克坦环,这对合成具有重大挑战.

研究的目的:

为了实现第一个全合成的广南氨酸A.
探索合成策略来构建紧张的麦克罗拉克坦核和安装关键的功能组.

主要方法:

催化闭环基基转化 (RCAM) 用于麦克罗拉克坦的形成.
催化氧化还原异构化,将普罗帕尔基酒精转化为一个enone.
为了引入外甲基组而修改过的彼得森化.
压力驱动的提亚迈克尔添加和随后的乙烯转化用于二硫化物部分装置.

主要成果:

成功合成了具有良好的整体产量的赛血基纳米辛A酒精.
在紧张的脚手架上展示关键的C-C和C-S键形成反应.
由于脚手架的敏感性,在最后的氧化步骤中遇到的挑战.

结论:

报告的综合体代表了获得复杂,紧张的自然产品的重大进步.
开发的合成途径为进一步探索广南氨酸A类似物提供了一个有价值的平台.
紧张的麦克罗拉克坦核心的敏感性限制了进一步的功能化,突出了独特的化学特性.

关键词:

基基因转基因发生.抗癌剂抗癌剂抗癌剂宏观循环是一种宏观循环.电解氧化异构化电解氧化异构化戒指应变应变应变

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