发现 N-(萘-1-基)-N'-烷基草酰胺配体能够实现铜催化的高转化率芳基胺化反应。
Discovery of N-(Naphthalen-1-yl)-N'-alkyl Oxalamide Ligands Enables Cu-Catalyzed Aryl Amination with High Turnovers.
机构信息
Interdisciplinary Center on Biology and Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 26 Qiuyue Lu, Shanghai 201210, China.
State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Lu, Shanghai 200032, China.
出版信息
Org Lett. 2017 Jun 2;19(11):2809-2812. doi: 10.1021/acs.orglett.7b00901. Epub 2017 May 22.
A class of N-(naphthalen-1-yl)-N'-alkyl oxalamides have been proven to be powerful ligands, making a coupling reaction of (hetero)aryl iodides with primary amines proceed at 50 °C with only 0.01 mol % of CuO and ligand as well as a coupling reaction of (hetero)aryl bromides with primary amines and ammonia at 80 °C with only 0.1 mol % of CuO and ligand. A wide range of coupling partners work well under these conditions, thereby providing an easy to operate method for preparing (hetero)aryl amines.
一类 N-(萘-1-基)-N'-烷基草酰胺已被证明是有效的配体，使（杂）芳基碘化物与伯胺在 50°C 下进行偶联反应，仅需 0.01 mol%的 CuO 和配体，以及（杂）芳基溴化物与伯胺和氨在 80°C 下进行偶联反应，仅需 0.1 mol%的 CuO 和配体。在这些条件下，各种偶联试剂都能很好地反应，从而为制备（杂）芳基胺提供了一种易于操作的方法。
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