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Ultrasound assisted synthesis of 2, 4-substituted 1, 5- benzothiazepine derivatives
* 1 , 2 , 3 , 4
1  Department Of Pharmaceutical Chemistry, R. C. Patel Institute Of Pharmaceutical Education & Research, Shirpur-425405, Dhule (M.S.) India
2  MVP’s Institute of Pharmaceutical Sciences, Adgoan, Nashik-422003 (M.S.) India
3  Wilson college, Girgaon Chawpatty,Mumbai 400007 , Maharashtra, India
4  Departamento de Química Orgánica, Facultad de Ciencias, Universidad of Santiago De Compostela, Alfonso X el Sabio, Lugo 27002, Spain


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.

Keywords: Green chemistry; ultra-sonication; Chalcone; Anticonvulsant