Description
Fleroxacin is a new, once daily trifluoroquinolone antibacterial structurally related to
norfloxacin. Available in both oral and IV formulations, it is reportedly useful in the
treatment of gonorrhea, bacterial enteritis, chronic bronchitis and urinary tract
infections. Fleroxacin has a longer serum half-life (9-12 hours) than other drugs of this
class, such as ciprofloxacin, enoxacin and norfloxacin.
Chemical Properties
White Needle-Like Crystals
Originator
Kyorin (Japan)
Definition
ChEBI: A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-n
gative bacteria.
Manufacturing Process
6,8-Difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-
oxoquinoline-3-carboxylic acid hydrochloride:
A mixed solution of 1-methylpiperazine (0.34 g) and pyridine (3 ml) was
added to 6,7,8-trifluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxoquinoline-3-
carboxylic acid (0.12 g) and heated to reflux for 6 hours. After the solvent
evaporated and cooled, the residue was adjusted to pH 1 with aqueous
hydrochloric acid. The cooled mixture was filtered off and the solid
recrystallized from water to give 6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-
(4-methyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid hydrochloride (0.08
g), melting point 269-271°C (decomp.).
Therapeutic Function
Antibacterial
