A Facile Access to Enantioenriched Isoindolines <i>via</i> One-Pot Sequential Cu(I)-Catalyzed Asymmetric 1,3-Dipolar Cycloaddition/Aromatization

Facile access to enantioenriched isoindolines bearing a quaternary stereogenic center and a tertiary stereogenic center was successfully developed via highly efficient Cu(I)/(S,Rp)-PPFOMe-catalyzed asymmetric 1,3-dipolar cycloaddition of azomethine ylide with quinone derivatives followed by silica-gel-promoted aromatization in a one-pot reaction protocol. The present catalytic system exhibited high diastereoselectivity, excellent enantioselectivity, and a broad substrate scope under mild conditions.本研究通过高效铜(I)/(S,Rp)-PPFOMe催化的亚胺叶立德与醌类衍生物的不对称1,3-偶极环加成反应，结合硅胶促进的芳构化一锅法策略，成功实现了兼具季碳手性中心与叔碳手性中心的对映体富集异吲哚啉的便捷合成。该催化体系在温和反应条件下，展现出优异的非对映选择性、卓越的对映选择性以及宽泛的底物适用范围。