Dzyubenko S. Synthesis, structure, physical, chemical and biological properties of 4-hydroxy-1-methyl-2,2-dioxo-1H-2?6,1-benzothiazine-3-carboxylic acid derivatives.

The thesis deals with the search of new biologically active substances among 4-hydroxy-1-methyl-2,2-dioxo-1H-2?6,1-benzothiazine-3-carboxamides. The preparatory method for obtaining methyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2?6,1-benzothiazine-3-carboxylate has been developed. Based on it a new scheme for the synthesis of hetaryl-, aryl- and arylalkylamides has been proposed. Structure has been confirmed by elemental analysis, NMR 1Н and 13С spectra, mass spectra, and in some cases by X-ray diffraction analysis. The analgesic activity of all substances synthesized and the diuretic properties of anilides have been studied. It has allowed to reveal interesting structural and biological regularities and recommend N-(5-chloropyridin-2-yl)-4-hydroxy-1-methyl-2,2-dioxo-1H-2?6,1-benzothiazine-3-carboxamide as a promising analgesic of a new chemical class for further research.