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Over the last few years research in the area of heterocyclic chemistry has become more and more important due to its usefulness of society. This chapter contain synthesis of pyriod-pyrimidine derivative having Thiourea as side chain substitution. This book mainly focused on various substitutions like Methyl, Methoxy, Nitro, Chloro, Fluoro and check their relative activity against various microbial. This book is useful for research students for whoever work in the field of synthetic chemistry.