通过/光电双催化实现的三元二碳功能化
Mark W Campbell1, Jordan S Compton1, Christopher B Kelly2,3
1Roy and Diana Vagelos Laboratories, Department of Chemistry , University of Pennsylvania , 231 South 34th Street , Philadelphia , Pennsylvania 19104-6323 , United States.
Journal of the American Chemical Society
|December 14, 2019
概括
一种新的光催化方法可以使用Giese类型的添加和Ni/photoredox双催化来实现olefins的二碳功能化. 这种方法在温和条件下有效地产生复杂的分子,包括四级和三级中心.
科学领域:
- 有机化学
- 催化剂
- 合成方法
背景情况:
- 在有机合成中,开发高效的素功能化方法至关重要.
- 传统的方法往往缺乏选择性或需要严苛的条件.
- 摄像和双催化为新的转化提供了有前途的途径.
研究的目的:
- 开发一种新的分子间光催化二碳功能化 (DCF).
- 将Giese类型的添加与Ni / photoredox双催化融合,以提高反应性和选择性.
- 能够合成具有四级和三级中心的复杂分子.
主要方法:
- 使用Giese型基质加和Ni/光双催化的组合.
- 用于区域选择性添加基的3°基.
- 针对轻度和功能组耐受性的最佳反应条件.
主要成果:
- 取得了成功的分子间光催化二碳功能化.
- 证明了烯的区域选择性化和化.
- 可以在一个步骤中安装四级和三级碳中心.
- 显示了与各种功能组的兼容性,包括皮纳科尔博酸.
- 应用了合成临床前候选剂 (TK-666) 的方法.
结论:
- 开发的双催化方法为olefin二碳素功能化提供了一个有效的途径.
- 这种方法允许在温和条件下构建复杂的分子结构.
- 该方法具有药物发现和开发的潜力,其在合成临床前候选中间体中的应用证明了这一点.
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