3-Aryl-4-aminomaleimides have well-demonstrated applications, such as use as fluorophores and inhibitors. However, their previous synthesizing methods are comprised of tedious multi-step procedures or methods that need to pre-functionalized maleimides, using toxic or unstable regents. Here, a feasible method is developed to synthesize these useful compounds. This includes the one-pot preparing 3-aminomaliemides, followed by the direct arylation of them through the palladium-catalyzed Heck reaction with various aryl iodides regiospecifically at the β position of their amine substituents. The results show this method efficiently provides a broad scope.

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