Chemoselective Oxypalladation of o‐Alkynyl Arylamides Triggered Site‐Selective C–H Annulation for Stereoselective Synthesis of Succinimide Fused Polycycles

We report herein a palladium‐catalyzed, site‐selective cyclative annulation of o‐alkynyl arylamides with maleimide for the stereoselective construction of succinimide‐incorporated benzoxazine derivatives. This operationally simple and modular protocol provides access to polycyclic frameworks. The other associated features are high functional group compatibility, gram‐scale synthetic potential, and downstream transformations. Control and labeling experiments were conducted to get insights into the mechanism.