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Synthesis And 5-HT2A Antagonist Activity Of Some 7-(3-(Substituted Amino) Propoxyl)-4- Methyl Chromen-2-Ones

Author(s): M. V. L Aparna, N Sati, V. S Veer, S. H Bhosale, M. S Bhosale, S. L Bodhankar, K. R Mahadik, S. S Kadam

Resorcinol on reaction with ethylacetoacetate in the presence of concentrated sulphuric acid afforded 7-hydroxy-4-methyl chromen-2-one (1), which when refluxed with 1-bromo-3-chloropropane in acetonitrile and in the presence of anhydrous potassium carbonate yielded 7-(3-chloropropoxyl)- 4-methyl chromen-2-one (2). Substitution of chlorine from (2) with secondary amines in toluene and in the presence of triethylamine resulted in the title compounds (3a-e) in 50-60 % yield. Their chemical structures have been assigned by elemental analysis , IR ,and 1HNMR analyses. The compounds were screened for 5-HT2A antagonist activity and spontaneous motor activity. All title compounds have been found to show significant 5-HT2A antagonist activity and caused reduction in spontaneous motor activity.


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