1. The pharmacokinetics and disposition of delafloxacin was investigated following a single intravenous (300 mg, 100 µCi) dose to healthy male subjects. 2. Mean Cmax, AUC0-∞, Tmax and t1/2 values for delafloxacin were 8.98 µg/mL, 21.31 µg h/mL, 1 h and 2.35 h, respectively, after intravenous dosing. 3. Radioactivity was predominantly excreted via the kidney with 66% of the radioactive dose recovered in the urine. Approximately 29% of the radioactivity was recovered in the faeces, giving an overall mean recovery of 94% administered radioactivity. 4. The predominant circulating components were identified as delafloxacin and a direct glucuronide conjugate of delafloxacin.
3,4,5,6,7-Pentaacetoxy-D-gluco-1-nitro-1-heptene with methanolic ammonia afforded crystalline 2-acetamido-1,2-dideoxy-1-nitro-D-glycero-D-gulo-heptitol which was converted via a modified Nef reaction to 2-acetamido-2-deoxy-D-glycero-D-gulo-heptose.
A new synthesis of 3-acetamido-3-deoxy-d-glucose (kanosamine) has been devised, involving the replacement by azide ion, with inversion, of the sulfonate group in 1,2;5,6-di-O-isopropylidene-3-O-p-tolylsulfonyl-d-allofuranose.
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