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Pyrimidine heterocycles are proven to be biologically active heterocycles, found in many biological systems, displaying a broad spectrum of biological activities including anticancer, anxiolytic, antioxidant, antiviral, antifungal, anticonvulsant, antidepressant and antibacterial activities. Recently, various synthetic approaches, synthetic strategy, the variation of substrates and study devoted towards the evaluation of biological activities for the pyrimidine heterocycles have been reported in the literature. This review article describes the synthesis of various biologically interesting pyrimidine heterocyclic ring systems using various nitrogen building blocks.