Direct and Practical Synthesis of Primary Anilines through Iron-Catalyzed C–H Bond Amination
作者:Luca Legnani、Gabriele Prina Cerai、Bill Morandi
DOI:10.1021/acscatal.6b02576
日期:2016.12.2
The direct C–H amination of arenes is an important strategy to streamline the discovery and preparation of functional molecules. Herein, we report an operationally simple arene C–H amination reaction that, in contrast to most literature precedent, affords directly the synthetically versatile primary aniline products without relying on protecting group manipulations. Inexpensive Fe(II)-sulfate serves
芳烃的直接C–H胺化是简化功能分子的发现和制备的重要策略。在本文中,我们报道了一种操作简单的芳烃CH胺化反应,与大多数文献先例相反,该反应直接提供了合成通用的伯胺产品,而无需依赖于保护基团的操纵。廉价的硫酸铁(II)可作为转化的方便催化剂。该反应可耐受多种芳烃,包括结构复杂的药物。重要的是,芳烃底物在转化中用作限制性试剂。这种操作上简单的转变将大大加快药物和功能分子的发现。