使用U形模板的Pd(II) 催化后的基甲烯酸化,化和氧化印林
Guoqiang Yang1, Petra Lindovska, Dajian Zhu
1Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Journal of the American Chemical Society
|July 10, 2014
概括
新的方法允许使用化模板对印度林的元选择性CH功能化. 这种方法克服了富含电子的基底的挑战,允许在特定的元位置修改多种不同的印丁衍生物.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 合成方法论 合成方法论
背景情况:
- 印度林是药物化学中重要的异环化合物.
- 直接的C-H功能化提供了高效的合成路线.
- 富含电子的印丁线通常在para-position处经历电友置换.
研究的目的:
- 开发新的方法,用于Indolines的元选择性CH功能化.
- 为了使复杂的印度类型的合成.
- 为了克服印度C-H激活中的区域选择性挑战.
主要方法:
- 使用了含有亚的模板,通过硫胺链接连接到印度林.
- 采用了一种单一保护的氨基酸连接体和催化剂的组合.
- 开发了元-C-H的olefination, arylation 和acetoxylation反应.
主要成果:
- 在C-H功能化中实现了高的元选择性. 富含电子的indolines.
- 成功地功能化了广泛的合成重要的印度类型.
- 证明了烯模板和氨基酸连接体在指导区域选择性方面的关键作用.
结论:
- 开发的方法提供了一个强大的工具,用于indolines的元选择性C-H功能化.
- 这一策略使得人们能够获得以前具有挑战性的印度林衍生品.
- 化模拟方法为印度多元化提供了一个多功能平台.
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