Title: Sitafloxacin
CAS Registry Number: 127254-12-0
CAS Name: 7-[(7S)-7-Amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Manufacturers' Codes: DU-6859
Molecular Formula: C19H18ClF2N3O3
Molecular Weight: 409.81
Percent Composition: C 55.69%, H 4.43%, Cl 8.65%, F 9.27%, N 10.25%, O 11.71%
Literature References: Fluorinated quinolone antibacterial. Prepn: I. Hayakawa, Y. Kimura, EP 341493; eidem, US 5587386 (1989, 1996 both to Daiichi); Y. Kimura et al., J. Med. Chem. 37, 3344 (1994). Antibacterial spectrum: L. M. Deshpande, R. N. Jones, Diagn. Microbiol. Infect. Dis. 37, 139 (2000). HPLC determn in serum and urine: H. Aoki et al., J. Chromatogr. B 660, 365 (1994). Clinical pharmacokinetics: M. Nakashima et al., Antimicrob. Agents Chemother. 39, 170 (1995). Clinical evaluation: N. Shetty, A. P. R. Wilson, J. Antimicrob. Chemother. 46, 633 (2000).
Derivative Type: Sesquihydrate
CAS Registry Number: 163253-35-8
Manufacturers' Codes: DU-6859a
Properties: Crystals from ethanol, water + ammonium hydroxide, mp 225° (dec). [a]589 -199.9° (c = 1 in 1 N NaOH). Soly in water: 131 mg/ml.
Melting point: mp 225° (dec)
Optical Rotation: [a]589 -199.9°
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs. |