Divergent One‐Pot Two‐Step Synthesis of Phosphoryl‐Substituted 4‐Quinolones and 3‐Indolinones

Herein, an approach is developed for the selective two‐step synthesis of phosphoryl‐substituted 4‐quinolones and phosphoryl‐substituted 3‐indolinones. This is achieved through the reaction of (3‐(2‐iodoaryl)‐3‐oxoprop‐1‐yn‐1‐yl)phosphonates with anilines followed by Cu‐catalyzed intramolecular cyclization of the intermediately formed regioisomeric enamines, which are selectively formed under neat conditions or in the presence of a gold complex as a catalyst. This method allows for the synthesis of a series of phosphoryl‐substituted 4‐quinolones and phosphoryl‐substituted 3‐indolinones in good yields.