Pazufloxacin , 98% , 127045-41-4

CAS NO.：127045-41-4

Empirical Formula: C16H15FN2O4

Molecular Weight: 318.3

MDL number: MFCD00865012

EINECS: 635-036-1

PRODUCT Properties

• Melting point: 269-271°C
• alpha: D25 -88.0° (c = 0.5 in 0.05N aq NaOH)
• Boiling point: 531.5±50.0 °C(Predicted)
• Density: 1.56
• storage temp.: 2-8°C
• solubility: Aqueous Base (Slightly, Sonicated), DMSO (Slightly, Heated), Methanol (Slightly)
• pka: 5.05±0.40(Predicted)
• color: Off-White to Pale Yellow

Description and Uses

Pazufloxacin is a novel quinolone marketed for the treatment of bacterial infections in Japan. This tricyclic fluoro-quinolone can be synthesized in 11 steps from commercially available 2,3,4,5tetrafluorobenzoic acid. The cyclopropyl substituent is first introduced in 6 steps including 4-F-substitution with tert-butylcyanoacetate, decarboxylation, aa alkylation with 1 ,Zdibromoethane, partial nitrile hydrolysis and Hoffmann-rearrangement. The pyridoxazine ring is then introduced in 5 steps including 6-ketoester formation and pryridoxazine annulation. Pazufloxacin displays a broad spectrum activity against Grampositive and Gram-negative bacteria, although it is less active that ciprofloxacin against pneumococci and is not active against ciprofloxacin-resistant isolates. In patients with gonococcal urethritis a high prevalence of fluoroquinolone-resistant N. gonorrhoeae isolates with the Ser-91-to-Phe mutation in GyrA was observed. However, good clinical responses have been seen in clinical trials of patients with urinary tract infections and to a lesser extent with respiratory tract infections. Pazufloxacin is mainly excreted in urine with a short half-life (2-2.5 h). It has a phototoxicity equal to that of ciprofloxacin and its adverse effect profile resembles that of other quinolones.

Pazufloxacin is a potential antimicrobial and/or antiviral agent.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302+H312+H332
• Precautionary statements: P261-P264-P280-P301+P312-P302+P352+P312-P304+P340+P312
• Hazard Codes: Xn,C,F
• Risk Statements: 20/21/22-34-11
• Safety Statements: 36/37-45-36/37/39-26-16
• WGK Germany: 3
• RTECS: UU8815300
• Toxicity: LD50 i.v. in male mice: >500 mg/kg (Todo)