Heterocyclic compounds play an important role as the main sources of lead molecules of agrochemicals. The 1,3,4-thiadiazinan-5-one nucleus is one of the most important and well known heterocyclic nuclei, which is a common and integral feature of a variety of natural products and medicinal agents. To find the novel lead compounds with various biological activities a series of thiadiazinan-5-one were rationally designed and synthesized. In this study an effort is made to synthesize 1,3,4-Thiadiazinan-5-one derivatives through the condensation reaction of Aryl aldehydes, substituted hydrazine derivatives and thioacetic acid using green solvent which is an efficient, green and facile three-component reaction. Using this method, 80% yield of thiadiazinan-5-one was obtained, while in conventional method, the yield only exceeded upto 50%. The chemical structures of the synthesized
compounds were characterized by considering the data of their elemental analysis as well as their spectral data using, FT-IR, 1H-NMR, 13C-NMR and Mass spectra. The compounds are found to possess good biological activity. Especially, compounds were bearing the sulfur and nitrogen atoms showed activity than those bearing the oxygen atom.