Pd(II)‐Catalyzed [3+2] Annulation of N‐Aryl‐2‐aminopyridines and Alkynes toward N‐(2‐Pyridyl)indoles

Abstract A Pd‐catalyzed formal [3+2] oxidative annulation of N‐aryl‐2‐aminopyridines and alkynes through pyridyl group directed C−H activation has been developed. This methodology provides a mild and atom‐economic approach for the efficient synthesis of highly substituted indoles in moderate to good yields, which features with mild reaction conditions, good functional group compatibility, operational simplicity and easy scale‐up.