总合成 (+) - 桑氨酸A 的合成
Amos B Smith1, Shuzhi Dong, Jehrod B Brenneman
1Department of Chemistry, Laboratory for Research on the Structure of Matter, and Monell Chemical Senses Center, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA. smithab@sas.upenn.edu
Journal of the American Chemical Society
|August 12, 2009
概括
复杂的宏类抗生素 (+) - - 桑素A 的总合成现在已经完成. 这一突破利用了先进的合成策略来构建复杂的分子,克服了重大的化学挑战.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 自然产品的合成自然产品的合成
背景情况:
- (+) - 索朗基辛A是一种复杂的类抗生素,具有显著的治疗潜力.
- 之前的努力受到分子复杂的结构和敏感的功能组的阻碍.
研究的目的:
- 为了实现第一个 (+) - - 桑素A的全合成,A.
- 开发和应用新型合成方法来构建复杂的自然产品.
主要方法:
- 采用了一种高度融合的合成策略,涉及三种先进碎片的合.
- 关键反应包括两种朱莉亚-科西恩斯基对立体选择性碎片结合的olefinations.
- 对于后期组装来说,A Stille合和Mukaiyama宏观培养是非常重要的.
- 使用精心控制的去保护步骤来保护敏感的 (Z,Z,E) -三酸连接.
主要成果:
- 首次成功完成 (+) - 桑亚基辛A的总合成.
- 在Julia-Kociénski的olefinations中实现了高E类固醇选择性.
- 合成途径有效地管理了微妙的 (Z,Z,E) -三酸盐部分,防止异构化或降解.
结论:
- 已经克服了 (+) - 桑素A 的合成挑战.
- 这种合成提供了一条可行的途径来获得这种重要的抗生素.
- 开发的方法可以应用于合成其他复杂的自然产品.
更多相关视频
相关概念视频
Combined Effects of Drugs: Synergism
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
Production of Antibiotics
Penicillin, one of the earliest and most widely used antibiotics, is produced industrially by the filamentous fungus Penicillium chrysogenum. Large stirred-tank bioreactors ranging from tens to hundreds of thousands of liters maintain tightly controlled temperature, pH, and dissolved oxygen conditions to support fungal metabolism and maximize antibiotic yield. Penicillin is a secondary metabolite, synthesized primarily during the stationary growth phase, which requires a carefully managed...


![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)