SYNTHESIS OF NEFOPAM ANALOGUES AND CHARACTERISATIONAbstract
Modified Benzoxazocine moiety of Nefopam with N-Protected-ethanolamine, fluorobenzene benzylbromide, 2,3-dimethyl-benzene, naphthalene, fluro-naphthalene. In these modification Friedel Craft alkylation plays vital role with using grignard reagent and aluminum chloride with the starting phthalic anhydride to form acid compound and was converted to amide compound with using of thionyl chloride, N-Protected ethanol amino and further converted to benzhydrol follows two synthetic routes, one routes is amide is converted to choro intermediate with thionyl chloride and then converted to benzhydrol, and another route is amide compound is directly converted into benzhydrol. Benzhydrol is the key intermediate for the preparation of all Nefopam analogs. These benzhydrol is undergone cyclization with p-Toluene sulfonic acid to forms benzoxazocine moiety of Nefopam analogs, by these ways disclosed nefopam analogs containing Benzoxazocine moiety as a novel analgesic therapeutic compounds, and these compounds were characterized by IR, 1H NMR Mass analysis.
K. Srinivasachary *, S. Tiwari, Y. S. Somannavar and B. Ramadevi
Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Indrakaran, Sangareddy, Telangana, India.
30 January 2019
21 July 2019
20 September 2019
01 October 2019