| 摘要 |
NEW MATERIAL:A compound of formula I [R<1> is H, alkyl, phenyl which may be substituted;R<2> is H, alkyl;formula II is cyclic amine which may be substituted and may include N, S and O atoms] and its salts. EXAMPLE:6,8-Difluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazet[ 3,2- a]quinoline-3-carboxylic acid ethyl ester. USE:Antibacterial against Pseudomonas aeruginosa, gram-positive bacteria and gram-negative bacteria. It has low toxicity. It can be used as a therapeutic agent for systemic infection and local infection such as urinary tract infection or biliary tract infection. PREPARATION:The cyclization reaction between a compound of formula III (R<3> is alkyl) and a dihalide of formula IV (Y, Z are halogen) such as methylene iodide is carried out in an inert solvent, in the presence of an acid acceptor at 0-120 deg.C. The compound of formula II, as a starting substance is novel. |
