| 摘要 |
Piperazinylquinoline-3-carboxylic acid derivs. of formula(I) [R1=alkyl, CH2: CH, 2-HOCH2CH2, FCH2CH2; R1, R3, R4=H or alkyl; R5=alkyl; R6=H or F are prepd. Thus, 15.0g 7-chloro-1-ethyl6- fluoro-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid and 16.7g 2- methyl piperazine are refluxed in pyridine and the residues are theated with ethanolic HCl to give 8.19g 1-ethyl-6-fluoro-1, 4- dihydro-7-(3-methyl-1-piperazinyl)-4-oxoquinoline-3-carnboxylic acid. HCl (I) are used as antibacterials which are more active than the known cpds. pipemedic acid and norfloxacin, with rapid urinary excretion and low toxicity.
|
