Copper‐Catalyzed Carbocyclization of Silyl Enol Ether Tethered Ynamides for Efficient and Practical Synthesis of 2‐Azabicyclo[3.2.0] Compounds†.

Summary of main observation and conclusion: An efficient copper‐catalyzed carbocyclization of silyl enol ether tethered ynamides has been developed, allowing rapid and practical construction of diverse 2‐azabicyclo[3.2.0] compounds in generally good to excellent yields with broad substrate scope under mild reaction conditions. Importantly, this protocol not only constitutes a rare example of non‐noble metal‐catalyzed alkyne carbocyclization, but also represents a rare cyclization on the β‐position of π‐tethered ynamides. The possibility of asymmetric carbocyclization via kinetic resolution also emerges. [ABSTRACT FROM AUTHOR]