通过C-H功能逻辑可扩展到阿里洛米辛
David S Peters1, Floyd E Romesberg1, Phil S Baran1
1Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Journal of the American Chemical Society
|January 31, 2018
概括
研究人员开发了一种新的简化合成阿里洛米抗生素. 这种方法使用铜介导的氧化联接来实现高效的宏循环,使这些有前途的抗菌剂更容易获得.
科学领域:
- 医学化学
- 有机合成
- 自然产品
背景情况:
- 阿里洛米辛是临床前开发中的强效抗菌天然产品.
- 现有的合成途径复杂,昂贵,并且需要大量时间进行扩展.
- 为了进一步的研究,简化对阿里洛米类型的获取至关重要.
研究的目的:
- 开发一种简化合成途径以获得阿里洛米辛类型.
- 能够扩展这些有前途的抗菌剂的生产.
- 合成和评估新型的阿里洛米辛类似物.
主要方法:
- 铜介导氧化合用于宏循环.
- 用于简化合成的C-H功能逻辑.
- 格拉姆尺度合成和阿里洛米辛的正式总合成.
主要成果:
- 建立了一个新的,操作简单的,可扩展的合成路线.
- 实现了同类规模最大的宏观循环.
- 一系列新的阿里洛米辛类似物被合成并进行生物评估.
结论:
- 新的合成策略大大简化了阿里洛米辛类似物的生产.
- 这种方法有助于开发新型抗菌剂.
- 该方法可用于临床前开发的大规模合成.
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