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2,1-BENZOTHIAZINE-2,2-DIOXIDES. 4. SYNTHESIS, STRUCTURE, AND ANALGESIC PROPERTIES OF 4-HYDROXY-1-METHYL-N-(PYRIDIN-2-YL)-2,2-DIOXO-1H-26,1-BENZOTHIAZINE-3-CARBOXAMIDES

И. В. Украинец, Л. А. Петрушова, С. П. Дзюбенко, Л. Янян
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Abstract


An improved method for the reaction of methyl-4-hydroxy-1-methyl-2,2-dioxo-1Н-2λ6,1-benzothiazine-3-carboxylate with hetaryl amines, which allows to obtain 4-hydroxy-1-methyl-2,2‑dioxo-N-(pyridin-2-yl)-1Н-2λ6,1-benzothiazine-3-carboxamides in good yields and with high purity. It was shown by x-ray analysis that the synthesized compounds exist in the zwitter-ion form. The mass spectra indicate their propensity to SO2 extrusion. In the pharmacological tests, rpomising compounds were found with analgesic activities exceeding those of known oxicam type drugs.

How to Cite
Ukrainets, I. V.; Petrushova, L. A.; Dzyubenko, S. P.; Liu Yangyang Chem. Heterocycl. Compd. 2014, 50, 564. [Khim. Geterotsikl. Soedin. 2014, 614.]

For this article in the English edition see DOI 10.1007/s10593-014-1508-1


Keywords


amides; 2-aminopyridine; 2-aminopyrazine; 2-aminopyrimidine; 2,1-benzothiazines; analgesic activity

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