One-pot, modular approach to functionalized ketones <i>via</i> nucleophilic addition/Buchwald–Hartwig amination strategy
作者:Jorn de Jong、Dorus Heijnen、Hugo Helbert、Ben L. Feringa
DOI:10.1039/c8cc08444k
日期:——
followed by the Buchwald–Hartwig amination with in situ released lithium amides is presented. In this work amides are used as masked ketones, revealed by the addition of organolithium reagents which generates a lithium amide, suitable for subsequent Buchwald–Hartwig coupling in the presence of a palladium catalyst. This methodology allows for rapid, efficient and atom economic synthesis of aminoarylketones
提出了一种一般的一锅法,将有机锂试剂1,2-添加到酰胺中,然后用原位释放的锂酰胺进行布赫瓦尔德-哈特维格胺胺化。在这项工作中,酰胺被用作掩蔽的酮,通过添加可生成锂酰胺的有机锂试剂揭示,该酰胺适合于随后在钯催化剂存在下进行的布赫瓦尔德-哈特维格偶联反应。该方法允许以良好的产率快速,有效和原子经济地合成氨基芳基酮。