Search for antitumor activity among derivatives of the 2,5-dihydropyrrole-2,5-dione

Metal‐Free, PhI(OAc)2‐Promoted Oxidative C(sp2)−H Difunctionalization: Synthesis of Thioaminated Naphthoquinones

“…In contrast, the addition of amine and thiol occurred sequentially with the nucleophilic substitution of 3,4dichloromaleimides. [53,54] In recent times, the intermolecular thioamination of maleimides has been reported with copper catalyst; otherwise, this type of direct coupling of maleimides with amines and thiols are very rare in literature. [55,56] In this work, we have observed that the thioamination of maleimide derivatives occurred with ease under the same standard conditions and notably, acetonitrile was found suitable as a solvent for this transformation (Table 3).…”

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

“…3‐amino‐4‐thiomaleimides are particularly important organic molecules due to their antibacterial and antitumor activities . Traditionally, they have been synthesized from the sequential nucleophilic substitution of 3,4‐dichloromaleimides with anilines and benzenethiols (Scheme a) . Moreover, the 3,4‐dichloromaleic anhydrides have also served as substrates to build 3‐amino‐4‐thiomaleimides in two steps, albeit with low yield (Scheme b) .…”