Synthesis, evaluation of analgesic and anti-inflammatory activities of substituted 1,2-benzoxazolone and 3-chloro-1,2-benzoxazole derivatives was written by Kiran, B. Ravi;Vijayakumar, G. R.;Bharath, H. S.;Sivakumar, R.;Sindhu, S.;Prakash, M. Shet. And the article was included in International Journal of Pharmaceutical Sciences and Research in 2015.Quality Control of 3-Chloro-6-methylbenzo[d]isoxazole The following contents are mentioned in the article:
Herein method for the synthesis of substituted 1,2-benzoxazolone I [R1 = H, NO2, Br; R2 = H, Me, F; R3 = H, NO2, F] and 3-chloro-1,2-benzoxazole derivatives II [R1 = H, NO2, Br; R2 = H, Me, F; R3 = H, NO2, F] was described. A new scheme was adapted for the construction of 1,2-benzoxazole ring from salicylic acid and its derivatives which leads to the formation of series of methyl-2-hydroxy-5-bromo benzoate, Me 2-hydroxybenzoates and N,2-dihydroxybenzamides substituted title compounds Synthesized compounds were characterized by IR, 1H-NMR and Mass spectral anal. Spectral data confirmed the compounds formation. Final compounds I and II were screened for their in-vivo analgesic activity by acetic acid induced writhing method in rats and anti-inflammatory activity by carrageenan-induced paw edema model. Among the compounds screened compound I [R1, R2, R3 = H] and compound II [R1, R2 = H; R3 = NO2] showed good analgesic activity of about 45% (writhing mean 8.9) and 54% (writhing mean 7.5) inhibition resp. at 5 mg/Kg po dosage. Compounds I [R1 = NO2; R2, R3 = H] and II [R1 = NO2; R2, R3 = H] (both having inhibition edema of 66.1%) showed significant anti-inflammatory activity. Other derivatives exhibited moderate to good analgesic and anti-inflammatory activities. This study involved multiple reactions and reactants, such as 3-Chloro-6-methylbenzo[d]isoxazole (cas: 16302-64-0Quality Control of 3-Chloro-6-methylbenzo[d]isoxazole).
3-Chloro-6-methylbenzo[d]isoxazole (cas: 16302-64-0) belongs to benzisoxazole derivatives. The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. Benzisoxazoles are found to display a variety of biological activities such as antiinflammatory, antioxidant, antidepressant, hypertensive, anticonvulsant, and anticoagulant properties.Quality Control of 3-Chloro-6-methylbenzo[d]isoxazole
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics