| 摘要 |
PURPOSE:To provide the subject new compound having excellent antibacterial activity and low toxicity and useful as an active component of antibacterial agent for the prevention and treatment of various infectious diseases. CONSTITUTION:The quinolinecarboxylic acid derivative of formula I [Z is group of formula II, formula III (R<1> is H, halogen, etc.), etc.] or its salt, e.g. 9,1-(methylimino)methano-7-fluoro-8-(2-methylmorpholino)-5-oxo-5H-thia zolo[3,2- a]quinoline-4-carboxylic acid. The compound can be produced by reacting a quinolinecarboxylic acid derivative of formula IV (R is H, lower alkyl, etc.) with a cyclic amine of formula ZH or its acid addition salt generally at a temperature between room temperature and 150 deg.C and, as necessary, hydrolyzing the product. The reaction of the compound of formula II with the amine of formula ZH is preferably carried out in a polar organic solvent (e.g. dimethyl sulfoxide) in the presence of an acid acceptor (e.g. triethylamine). |
