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一种模块化和对抗选择性合成的多菌素抗生素

Stephen K Murphy¹, Mingshuo Zeng¹, Seth B Herzon^2,3

¹Department of Chemistry, Yale University, New Haven, CT 06520, USA.

Science (New York, N.Y.)

|June 3, 2017

概括

一个新的模块化合成使得创建新型的肺素抗生素衍生物. 这种方法为开发改进的抗菌药物提供了更大的结构控制,包括那些对格兰氏阴性细菌有效的药物.

科学领域:

医学化学
有机合成
微生物学

背景情况:

一种真菌代谢物 (+) - 素是开发抗生素药物的关键原料.
之前的半合成修改产生了临床上有用的类似物和化合物,对抗了格兰氏阴性病原体.
半合成的局限性阻碍了优化抗生素特性的精确结构控制.

研究的目的:

开发一个模块化合成的 pleuromutilin衍生品与完整的结构控制.
能够制造出具有潜在改善抗菌作用的新型肺类药物.
克服传统半合成方法的局限性.

主要方法:

采用了一个融合合成策略.
关键反应涉及胺与双功能乙烯的结合.
通过制备五种特定的斑素衍生物来证明这种合成.

主要成果:

一种模块化合成途径成功地被确定为pleuromutilins.
合成提供了 (+) -12-epi-mutilin, (+) -11-12-di-epi-mutilin, (+) -12-epi-pleuromutilin, (+) -11-12-di-epi-pleuromutilin和 (+) -pleuromutilin.
在合理数量的步骤 (17到20) 中完成了合成.

结论:

开发的模块化合成为获取多种多样性肌蛋白结构提供了强大的工具.
这种方法有助于探索新型抗生素的结构-活性关系.
它提供了一种工程 pleuromutilin衍生品的途径, 具有对具有挑战性的细菌感染的潜在增强疗效.

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Regioselective Formation of Enolates

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As depicted in the figure below, the unsymmetrical ketones can form two possible enolates: less substituted or more substituted enolates. Usually, the thermodynamic enolates are formed from the more substituted α-carbon atom, while the kinetic enolates are formed faster by deprotonation from the less substituted position. The thermodynamic enolates have lower energy, so they are more stable. But the energy required to form kinetic enolates is less.