Copper‐Catalyzed One‐Pot Approach to 6‐Membered Sultams From Vinyl Sulfonamide Using Methanol as C1 Building Block

A CuBr ₂ ‐catalyzed one‐pot oxidative coupling of vinyl sulfonamides with methanol has been developed for the efficient construction of taurultams. Methanol functions dually as solvent and C1 source, while H ₂ O ₂ serves as a benign oxidant. The reaction proceeds under ambient conditions without inert atmosphere requirements, demonstrating excellent functional group tolerance and delivering diverse sultams in high yields. This operationally straightforward protocol demonstrates that copper‐catalyzed activation of methanol enables its utilization as a sustainable C1 building block for taurultam synthesis, establishing a scalable and practical route to 6‐membered sultam scaffolds.