C(sp2) -H 用稳定于空气的预催化剂对化的玻里化:电子增强的位点选择性使合成机会成为可能
Jennifer V Obligacion1, Máté J Bezdek1, Paul J Chirik1
1Department of Chemistry, Princeton University , New Jersey 08544, United States.
Journal of the American Chemical Society
|February 1, 2017
概括
新的催化剂在化的C(sp2) -H玻里化过程中实现了高的正正对的选择性. 这一突破使抗炎药物flurbiprofen的高效合成成为可能.
科学领域:
- 有机金属化学 有机金属化学
- 催化剂是一种催化剂.
- 合成有机化学 合成有机化学
背景情况:
- 化是有机合成中的一个关键反应.
- 在化烯的化过程中,实现位点选择性,特别是对的整形转化,是具有挑战性的.
- 贵金属催化剂通常依赖于指导组,限制基质范围.
研究的目的:
- 开发新的催化剂,用于化的选择性C ((sp2) -H玻利化.
- 为了实现高的正正对的选择性,覆盖了传统的定向组效应.
- 为了证明这些催化剂在合成有价值的制药化合物的实用性.
主要方法:
- 合成和表征含有4-Me-iPrPNP连接体的 (III) 二化玻利 (1) 和 (II) 双酸) (2) 复合体.
- 评估各种化的C(sp2) -H玻里化中的催化活性和选择性.
- 评估功能组耐受性和与其他试剂 (如氨基胺和西兰) 的兼容性.
主要成果:
- 开发电子增强的催化剂,在C ((sp2) -H玻利化过程中表现出高的对的选择性.
- 空气敏感的 (III) 和空气稳定的 (II) 催化剂都表现出广泛的功能组耐受性.
- 观察到的选择性即使在存在基二甲基胺和西兰,也保持,超过贵金属催化剂的性能.
- 催化系统成功地应用于flurbiprofen的高效合成.
结论:
- 新型催化剂为化的C ((sp2) -H玻利化提供了电子增强的位点选择性.
- 这些催化剂为贵金属系统提供了强大的替代品,克服了与指导组相关的局限性.
- 开发的方法促进了重要的分子的实际合成,包括抗炎药物flurbiprofen.
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