连接剂促进的C-H氨化和化
Peng Wang1, Gen-Cheng Li1, Pankaj Jain1
1Department of Chemistry, The Scripps Research Institute , 10550 N. Torrey Pines Road, La Jolla, California 92037, United States.
Journal of the American Chemical Society
|October 8, 2016
概括
研究人员开发了对氨酸和醇的新型C-H氨化和化方法. 这些转化利用了经过修改的诺波介质和独特的胺连接体,使多种基质,包括异态循环的有效功能化成为可能.
科学领域:
- 有机化学
- 催化剂
- 合成方法
背景情况:
- 与传统方法相比,直接的C-H功能化提供了更有效的合成途径.
- 在有机合成中,元选择性C-H功能化仍然是一个重大挑战.
- 素和衍生物是制药和材料科学的重要组成部分.
研究的目的:
- 为素和基材开发新型的C-H氨化和化反应.
- 引入一个暂时的调解器策略来挑战CH功能化.
- 建立适用于一系列芳香和异芳香化合物的多功能方法.
主要方法:
- 作为一种短暂的介质,使用了改性诺博伦 (甲基双环[2.2.1] -2-烯-2-碳酸盐).
- 使用专门设计的单一保护的3-氨基-2-氧胺/胺类型连接剂.
- 对甲胺和甲基化反应条件进行了研究.
主要成果:
- 实现了第一个报告的甲基C-H氨基化和甲基C-H化.
- 证明了广泛的基质范围,包括各种氨酸和衍生物.
- 已成功地将该方法应用于醇,醇和醇等异环基质,产生中等到高产量的产品.
结论:
- 开发的方法提供了前所未有的超功能化氨酸和.
- 修改后的诺波介质和皮里丁配体的组合是反应成功的关键.
- 这项工作扩展了C-H功能化的工具包,特别是对元选择性转换.
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