Gavin Joshua T, Anderson Lars W, Roberts Courtney C
Department of Chemistry, University of Minnesota─Twin Cities, Minneapolis, Minnesota 55455, United States.
Org Lett. 2024 Sep 13;26(36):7530-7534. doi: 10.1021/acs.orglett.4c02407. Epub 2024 Aug 28.
Methods for aryne difunctionalization have been the focus of recent research, but one limitation is the use of nucleophiles with proton sources. Herein, we demonstrate the use of halogen transfer reagents to enable protic amines in aryne aminohalogenation difunctionalizations in up to 86% yield. This method uses amines and arynes with a variety of N-heterocyclic scaffolds. Through a variety of derivatizations, the synthetic utility of these products is demonstrated.
芳炔双官能团化方法一直是近期研究的重点，但一个局限性是亲核试剂与质子源的联用。在此，我们展示了使用卤素转移试剂，使质子胺在芳炔氨卤化双官能团化反应中能达到高达86%的产率。该方法使用了带有各种N - 杂环骨架的胺和芳炔。通过各种衍生化反应，证明了这些产物的合成效用。
