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作为掩饰核友的二甲基组:一个易斯酸/基方法
Jacob B Geri1, Michael M Wade Wolfe1, Nathaniel K Szymczak1
1Department of Chemistry , University of Michigan , 930 N. University , Ann Arbor , Michigan 48109 , United States.
Journal of the American Chemical Society
|July 25, 2018
概括
研究人员开发了一种新方法来制造二甲基化合物, 这种方法利用超基和易斯酸产生反应性二甲基离子,使得新二甲基连接的合成成为可能.
科学领域:
- 有机化学
- 医学化学
- 合成化学
背景情况:
- 二甲基 (CF2H) 增强了药物的药理动力学特性.
- 现有的方法缺乏有效的途径来功能化Ar-CF2H原材料.
- 二甲基 (Ar-CF2-R) 连接在药物设计中具有价值.
研究的目的:
- 探索Ar-CF2H的去质子化以形成核友Ar-CF2合成子.
- 开发一种合成基Ar-CF2-R连接的一般方法.
- 在药物化学中提供传统基链接的替代品.
主要方法:
- 使用布伦斯特德超基和弱易斯酸的组合.
- 脱质Ar-CF2H以产生反应性的Ar-CF2片段.
- 在室温下,Ar-CF2-合成子与各种电友的反应.
主要成果:
- 成功解质并捕获Ar-CF2合成子.
- 通过各种电友和二甲基 (hetero) 氨基体证明了广泛的范围.
- 获得可分离和可反应的Ar-CF2合成子.
- 用于合成二甲连接的方法.
结论:
- 建立了二联结的新型和一般合成途径.
- 开发的方法为药物化学提供了有价值的工具.
- 这种方法为药物分子中的基提供了代谢稳定和脂性替代物.
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