abstract |
PURPOSE: To obtain a new thiazine or oxazine derivative excellent as a preventive and therapeutic agent for ischemic encephalopathy and/or cerebral nerve cytotoxicity. n CONSTITUTION: A compound, e.g. 3-(4-chlorophenyl)-1H-naphtho[2,1- b][1,4]thiazin-2(3H)-one expressed by formula I (R 1 and R 2 are H, lower alkyl, cycloalkyl, phenyl, etc.; A is lower alkylene; X is S or O; R 3 and R 4 are H, lower alkyl, lower alkenyl, etc.). The aforementioned compound is obtained by subjecting a compound expressed by formula II and an amine compound expressed by formula III (Y 3 is reactive residue) or its salt to condensing reaction in the presence or absence of a base (e.g. an alkali metallic carbonate) in or without a solvent (e.g. ethanol) at 0-150°C. The compound expressed by formula I is capable of directly acting on cerebral cells with hardly any action on cardiovascular systems. n COPYRIGHT: (C)1992,JPO&Japio |