Synthesis of Multisubstituted Pyranoindol‐1‐ones Using Iridium‐Catalyzed Intramolecular C─H Amination of 3‐Amino‐4‐phenyl‐2‐pyrones

Abstract A method for the synthesis of multisubstituted pyranoindol‐1‐ones is developed, utilizing iridium‐catalyzed intramolecular C─H amination of 3‐amino‐4‐phenyl‐2‐pyrones synthesized via the conjugate addition of diethyl 2‐aminomalonate to alkynyl ketones. This synthetic strategy was successfully applied to the synthesis of analogues of biologically active compounds.