Copper‐Mediated (2‐Methylthio)aniline Directed Annulation of sp2 C−H Bonds with Primary Anilines

Abstract A method for copper‐mediated, directed functionalization of sp 2 C−H bonds in benzamides with primary anilines toward synthesis of indazolones is reported. Successful transformations relied on the use of a bidentate 2‐methylthio aniline directing group. Functionalities including halogen, methylthio, cyano, ester, protected alcohol, and tertiary amine groups were compatible with reaction conditions. The method features a rare example for directed annulation of sp 2 C−H bonds with amines.