催化后期阶段的异质C-H亚化
Xiongyi Huang1, Tova M Bergsten1, John T Groves1
1Department of Chemistry, Princeton University, Princeton, New Jersey 08544 United States.
Journal of the American Chemical Society
|April 15, 2015
概括
这项研究引入了一种催化反应,用于使用水性酸将C-H键转化为酸. 这种高效的方法使生物活性分子的后期功能化成为可能,并证明了对C-H的酶化.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 药用化学 医学化学
背景情况:
- 阿利法性C-H键在有机分子中无处不在.
- 有机亚酸是合成中的多功能中间体.
- 对于C-H功能化的高效方法是非常受欢迎的.
研究的目的:
- 开发一种催化方法,用于亚利法性C-H亚化.
- 为了证明这种反应对生物活性化合物的后期功能化的有用性.
- 为了实现对抗选择性C-H亚化.
主要方法:
- 使用水性酸的催化反应.
- 在有氧条件下进行的反应.
- 适用于二级,三级和基C-H键.
主要成果:
- 能有效地将C-H键转换为亚化物,收益率高达74%.
- 成功的晚期阿齐达化药物,如普雷加巴林,孟坦丁和阿尔特米西宁.
- 在Mn-催化式的enantioselective亚化中达到70%的反体过量 (ee).
结论:
- 开发的Mn-azidation方法在操作上简单且高效.
- 这种方法对药物发现和化学生物学具有重大潜力.
- 酶选择性C-H亚化扩大了这种转换的合成效用.
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