<scp>Copper‐Catalyzed</scp> Carbocyclization of Silyl Enol Ether Tethered Ynamides for Efficient and Practical Synthesis of <scp>2‐Azabicyclo</scp>[3.2.0] Compounds^†

Abstract

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.

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