晚期芳香C-H氧化
Jonas Börgel1, Lalita Tanwar1, Florian Berger1
1Max-Planck-Institut für Kohlenforschung , Kaiser-Wilhelm-Platz 1 , D-45470 Mülheim an der Ruhr , Germany.
Journal of the American Chemical Society
|November 14, 2018
概括
我们开发了一种氧化芳香C-O键形成的新方法, 这种方法提供了很高的功能组耐受性,并通过安装C-F键来阻止代谢热点.
科学领域:
- 有机化学
- 医学化学
- 药物发现
背景情况:
- 氧化芳香C-O键形成的合成方法是有限的.
- 芳香C-O键的形成对合成药物代谢物很重要.
- 晚期功能化是药物发现和开发的关键.
研究的目的:
- 开发一种新的C-O键形成的新方法.
- 提供药物的潜在人体代谢物.
- 使用C-F键阻止代谢热点.
主要方法:
- 作为试剂使用了二甲硫氧化物.
- 在上进行氧化芳香C-O键形成.
- 研究功能组耐受性和化学选择性.
主要成果:
- 实现了新型的C-O键形成的后期阶段.
- 对高度功能化的基质表现出良好的功能群耐受性.
- 作为药物代谢物的前体和C-F键安装的生成的基酸盐.
结论:
- 开发的方法对于合成潜在的人类代谢物具有价值.
- 该方法允许通过安装C-F键来阻止代谢热点.
- 电荷转移相互作用可以解释反应的化学选择性.
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