Solvent-Free Buchwald-Hartwig Reaction of Aryl and Heteroaryl Halides with Secondary Amines
作者:Maxim A. Topchiy、Andrey F. Asachenko、Mikhail S. Nechaev
DOI:10.1002/ejoc.201402077
日期:2014.6
A highly efficient solvent-free protocol for the Buchwald–Hartwig amination of (hetero)aryl halides by secondary amines was developed. The reaction is mediated by a Pd(OAc)2/RuPhos catalytic system in air. Various (hetero)aryl halides were coupled with diaryl, alkyl–aryl, and dialkylamines in good to excellent yields (51 examples, 50–99 % yield).
开发了一种高效的无溶剂方案,用于通过仲胺对(杂)芳基卤化物进行 Buchwald-Hartwig 胺化。该反应由空气中的 Pd(OAc)2/RuPhos 催化系统介导。各种(杂)芳基卤化物与二芳基、烷基-芳基和二烷基胺以良好至极好的产率偶联(51 个实例,产率 50-99%)。