Rhodium(III)‐Catalyzed Three‐Component Cascade Annulation for Modular Assembly of N‐Alkoxylated 3‐Arylisoindolin‐1‐ones with Tetrasubstituted Carbon Center

A cascade C−H activation, annulation, and etherification of N ‐hydroxybenzamides with propargylamines provides a flexible route to N ‐alkoxylated 3‐arylisoindolin‐1‐ones. Three new bonds (C−C, C−N, and C−O) are generated to afford a series of isoindolin‐1‐ones bearing a tetrasubstituted carbon in 49–82% yield. The utility of this method was showcased by gram‐scale synthesis and synthetic transformations of the product to access structurally diverse isoindolinones. magnified image