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Abstract

Azauracils have been extensively studied for their clinical applications. For example, 6-azauracil and its derivatives have been extensively used in chemotherapy of cancer [1,2], inhibit viruses [3-5]. They are also used as a fungicide [6], chemotherapeutic agents for psoriasis [7], for polyarthritis [8] and for polycythemia vera [9]. It has been reported that 1-N position of 6-azauracil is served as the best location to place a substituent to mimic the size and shape of the natural nucleoside [10]. Attachment of substituted phenyl side chain at N-1 of 6-azauracil causes increasing its potency, which was related in part to the acidity of the imide hydrogen. Therefore, substituents attached at N-1 position will affect the pharmacokinetics and the binding properties of the drug. In addition, the polarizability of N-aryl-6-azauracil extends through out the molecule and leads adaptation to the active site [11], therefore N-aryl 6azauracil derivatives are biologically active molecules [12-15] (Fig. 1). Traditionally N-aryl 6-azauracil derivatives were synthesized [16] from corresponding anilines in 4 steps as shown in Scheme-I. However, used harsh reaction conditions and A Mild and Efficient Copper-Mediated N-Arylation of 6-Azauracil with Corresponding Boronic Acids and their Antibacterial Activity