H-Phosphonate-Mediated Amination of Quinoline N-Oxides with Trialkylamines

Chen, Zhao et al. have reported the H-phosphonate-mediated direct amination of quinoline N-oxides with trialkylamines. H-Phosphonate (diisopropyl phosphite) works as an efficient C-2-H activator of a quinoline moiety in the amination process, and the reaction successfully proceeds in one-pot under metal-free conditions at room temperature. They propose the reaction mechanism based on the monitoring results of the reaction process with ³¹P NMR. In this way, this synthetic method is expected to be useful for producing 2-dialkylaminoquinolines which are pharmaceutically important alkaloids.