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

Abstract C5-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 Introduction 2 Coupling of Prefunctionalized Uracils with (Hetero)aryl Reagents 2.1 Negishi Coupling 2.2 Suzuki–Miyaura Coupling 2.3 Stille Coupling 3 Coupling of Functionalized Uracils with Nonactivated Aromatic (Hetero)cycles 3.1 Photochemically Induced Coupling 3.2 Palladium-Catalyzed Coupling 4 Coupling of Nonactivated Uracil/Uridine with Functionalized Aromatic (Hetero)cycles 4.1 Electrochemical Reduction 4.2 Transition-Metal-Catalyzed Coupling 4.3 Light-Promoted Coupling of Uracils with Diazonium Salts 5 Direct Coupling of Nonactivated Uracils with Nonactivated Aromatic (Hetero)cycles 6 Summary and Prospects