一个光催化方法,激进的1- ((三甲基) cyclopropanation
Sven Timmann1, Moritz T H Dilchert1, Jörg Dietzel1
1Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstr 2, Göttingen 37077, Germany.
概括
一种新的试剂使得三甲基cyclopropyl组的多重组合成. 这种方法在温和条件下有效地将这种重要的化学结构纳入各种分子中,有助于药物发现.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 摄影化学的使用.
背景情况:
- 三甲基cyclopropyl组是医药化学的一个特权支架.
- 在药物发现过程中,将这一部分纳入有效的方法至关重要.
- 现有的方法通常需要恶劣的条件或具有有限的基质范围.
研究的目的:
- 开发一种简单且可扩展的协议,用于合成用于三甲基cyclopropanation的新型试剂.
- 为了证明这种试剂在将三甲基cyclopropyl组纳入各种有机分子中的实用性.
- 要突出试剂在制备医学上相关的构建块中的适用性.
主要方法:
- 在多重克尺度上合成5 - - - - - - - - - - - - - - - - 三甲基 (cyclopropyl) - - - - - - - 双三酸.
- 温和的光化学条件产生激素.
- 试剂应用于各种 (异质) 和乙醇乙烯.
主要成果:
- 这种基板稳定的试剂有效地释放了1-三甲基) cyclopropyl基.
- 在非功能化的位置直接纳入三甲基cyclopropyl 化学型.
- 实现了广泛的基质范围,优异的功能组耐受性,高区域选择性和有用的产量.
结论:
- 开发的协议提供了一种简单有效的三甲基cyclopropanation的方法.
- 该试剂非常适合合成医学上相关的构建模块.
- 这项工作扩大了合成工具箱,以获取有价值的化有机化合物.
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