Three‐Component Coupling Reactions of Maleimides, Thiols, and Amines: One‐Step Construction of 3,4‐Heteroatom‐functionalized Maleimides by Copper‐Catalyzed C(sp2)−H Thioamination

Abstract A copper‐catalyzed intermolecular thioamination of maleimides with thiols and amines has been developed. A diverse range of 3‐amino‐4‐thiomaleimides and 3,4‐dihydropyrrolo[3,4‐ b ][1,4]thiazine‐5,7(2 H ,6 H )‐diones were obtained with good yields, involving C−N and C−S bond formations. This methodology is very practical and features high atom economy, excellent functional group tolerance. magnified image