Regioselective arylation of uracil and 4-pyridone derivatives via copper(I) bromide mediated C-H bond activation

A facile and effective synthesis of 6-aryluracil derivatives was accomplished by the direct C-H bond activation for arylation. A series of 6-aryl-1,3-dimethyluracils were synthesized from the reaction of 1,3-dimethyluracil with various phenyl iodides in DMF, in the presence of copper(I) bromide as the catalyst and lithium tert-butoxide as the base. This methodology is applicable to a variety of 5-substituted uracils as well as 4-pyridone to provide direct accesses to versatile uracil and 4-pyridone derivatives.