DERIVATIVES OF BENZOXAZINE, METHODS OF THEIR SYNTHESIS, A PHARMACEUTICAL PREPARATION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of benzoxazine as an optically pure isomer or a mixture of optically pure isomers of the formula (I) where Y - hydrogen, fluorine, chlorine atoms, methyl- or methoxy-group; R₁ - phenyl substituted with fluorine, methyl, methoxy-, trifluoromethyl-group or phenyl or thiene-2-yl-group; R₂ - methyl; R₃ - alkyl, phenylalkyl possibly substituted with 2-3 methoxyl-groups or 2-(pyridine- -2-yl)-ethyl; or R₂ and R₃ with nitrogen atom form 4-phenyl- -(piperidine-1-yl), 4-phenylmethyl-(piperidine-1-yl), 1,2,3,4-tetrahydroisoquinoline-2-yl, 6-methoxy-1,2,3,4-tetrahydro-isoquinoline-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquino-line-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-yl, 2,3,4,5-tetrahydro-1H-3-benzazepine-3-yl, 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-3-yl; X - carbonyl- or sulfonyl-group, or their salts show in vitro properties of neurogenic calcium-antagonists and in vivo - neuroprotective and anti-ischemic properties. EFFECT: improved method of synthesis, neuroprotective and anti-ischemic properties. 5 cl, 1 tbl, 42 ex