在没有化物的情况下对素进行选择性化
Alexander W Schuppe1, Gustavo M Borrajo-Calleja1, Stephen L Buchwald1
1Department of Chemistry , Massachusetts Institute of Technology , 77 Massachusetts Avenue , Cambridge , Massachusetts 02139 , United States.
Journal of the American Chemical Society
|November 6, 2019
概括
这项研究引入了一种新的无化物方法,使用双/铜催化合成. 这种方法为有价值的药物中间体提供了更绿色的途径.
科学领域:
- 有机化学
- 催化剂
- 合成方法
背景情况:
- 在药物合成中,酸是非常重要的组成部分.
- 传统的化法通常涉及有毒的化物试剂.
- 开发高效和安全的替代品是有机合成的一个重大挑战.
研究的目的:
- 开发一种无化物协议,用于olefins的选择性化.
- 为了使马尔科夫尼科夫和抗马尔科夫尼科夫添加化物等价物.
- 提供一种通用的方法来获取缩.
主要方法:
- 采用了双Pd/CuH催化系统.
- 氧化被用作安全的化等效物.
- 进行了水利化,随后进行了 [4 + 2]/反向- [4 + 2] 解构序列.
主要成果:
- 实现了非对称的马尔科夫尼科夫化.
- 启用了终端油脂的抗马尔科夫尼科夫化.
- 在温和的反应条件下合成酸.
结论:
- 开发的协议提供了一种无化物和有效的途径,以获得有价值的化.
- 这种方法扩大了制药中间体的合成工具包.
- 使用氧化作为化替代品提供了比传统化来源更安全的替代品.
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