Recent Advances in the Synthesis of 5-(Hetero)aryl Uracil Derivatives

Abstract

AbstractC5-Aryl/heteroaryl uracil-based compounds have attracted continuous interest because of their wide biological potential. In this review, we outline the primary synthetic methods used to prepare designated uracils, various combinations of which have been used to synthesize target compounds with potential biological activities. The significance of each approach and its limitations are also summarized.1 Introduction2 Coupling of Prefunctionalized Uracils with (Hetero)aryl Reagents2.1 Negishi Coupling2.2 Suzuki–Miyaura Coupling2.3 Stille Coupling3 Coupling of Functionalized Uracils with Nonactivated Aromatic (Hetero)cycles3.1 Photochemically Induced Coupling3.2 Palladium-Catalyzed Coupling4 Coupling of Nonactivated Uracil/Uridine with Functionalized Aromatic (Hetero)cycles4.1 Electrochemical Reduction4.2 Transition-Metal-Catalyzed Coupling4.3 Light-Promoted Coupling of Uracils with Diazonium Salts5 Direct Coupling of Nonactivated Uracils with Nonactivated Aromatic (Hetero)cycles6 Summary and Prospects