Department of Chemistry, Xinjiang Normal University , Urumqi 830054, China.
Department of Chemistry, University of Science and Technology of China , Hefei 230026, China.
J Org Chem. 2016 Nov 18;81(22):11384-11388. doi: 10.1021/acs.joc.6b01772. Epub 2016 Nov 1.
A chiral phosphoric acid-catalyzed one-pot enantioselective reductive amination of 2-pyridyl ketones was realized to provide chiral pyridine-based ligands in excellent yields with high enantioselectivities (up to 98% yield, 94% ee). Computational studies on the key intermediate imine and transition state of the hydride transfer process revealed that the nitrogen atom of the pyridyl ring might be an important factor to significantly promote both the reaction activity and enantioselectivity.
手性磷酸催化的 2-吡啶酮一锅法对映选择性还原胺化反应实现了手性吡啶基配体的高产率和高对映选择性（高达 98%收率，94%ee）。对关键中间体亚胺和氢转移过程过渡态的计算研究表明，吡啶环的氮原子可能是显著提高反应活性和对映选择性的重要因素。
