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Late-stage functionalization of pyrido[1,2-a]pyrimidin-4-one at pyrimidine ring structure is crucial to design pharmaceuticals, agrochemicals and materials for sustainable development. 4H-pyrido[1,2-a]pyrimidin-4-ones skeleton, a potent privileged scaffold, ubiquitously exists in numerous bioactive natural and pharmacologic products. Scope of different synthetic methods including their synthetic application to design new materials and biological activity of differently substituted 4H-pyrido[1,2-a]pyrimidin-4-ones are of main interest. Researchers are relentlessly working to develop more efficient and ecofriendly methods for their synthesis. This review provides, a comprehensive discussion of the recent advancements in the field of synthesis and application of 3-hetero-substituted 4H-pyrido[1,2-a]pyrimidin-4-one for sustainable development.
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