Palladium‐Catalyzed Tandem 1,6‐Enyne Cyclization/Suzuki Reaction for the Synthesis of Diaryl Compounds

Comprehensive Summary Herein, it is reported that a palladium/bidentate amine ligand cooperative catalytic system has been developed to achieve the intramolecular cyclization of 1,6‐enyne coupled with a Suzuki cross‐coupling reaction, successfully constructing a diaryl‐substituted γ‐butyrolactam skeleton. The tandem catalytic mechanism significantly enhances synthetic efficiency by circumventing the isolation and purification of intermediates required in traditional stepwise synthesis, demonstrating exceptional step economy. This method provides a novel modular strategy for the rapid assembly of bioactive diaryl‐containing lactam compound libraries.