Abstract:A series of 15 novel derivatives of Synthesis of 2, 4-substituted 1, 5- benzothiazepine 5a–l were synthesized in good yield from the key compound 1, 3-substituted-prop-2-en-1-one (3a-l), called chalcone, with 2-aminothiophenol (0.01mol) and pinch of zirconium oxychloride and solvent dimethyl formamide (DMF), by using ultra-sonication as one of the green chemistry tools. All the synthesised compounds were evaluated for anticonvulsant activity. The synthesized derivatives were investigated for CNS depressant, maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening.