This review is an attempt to compile the literature of various synthetic procedures of pyrimidine analogs. Pyrimidine and its fused pyrimidine derivatives are a class of heterocyclic scaffolds that demonstrates a broad range of biological and pharmacological activities such as anticancer, anxiolytic, antioxidant, antiviral, antifungal, anticonvulsant, antidepressant, and antibacterial activities. According to World Health Organization reports, cancer remains a major cause of death in worldwide and there is a need to develop an effective drug against cancer. The literature indicated that pyrimidine motifs acts as anticancer agents, which motivates the researchers to design a series of pyrimidine heterocycles. © 2016, Copyright © Taylor & Francis Group, LLC.