Antimicrobial quinolones, their compositions and uses
a technology of quinolones and quinolonyls, applied in the field of quinolones and quinolonyl antimicrobial compounds, can solve the problems of defying the art accepted structure/activity relationship of quinolones and quinolonyl compounds, and achieve the effects of reducing toxicity, improving pharmacology, and low susceptibility to microbial resistan
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example a
Preparation of 7-[3R-(1-amino-methylethylpyrrolidinyl)]-1-cyclopropyl-1,4--dihydro-8-chloro-6-hydroxy-4-oxo-3-quinolinecarboxylic acid sulfate
[0106] Synthetic Pathway: 60
[0107] Procedures:
[0108] 3-Chloro-2,4-difluoro-bromobenzene
[0109] To a solution of 19 ml (0.135 mole) of diisopropylamine in 125 ml of tetrahydrofuran (THF) cooled at -20.degree. C. is added 80 ml of n-butyllithium (1.6 M in hexane). The temperature is raised to 0.degree. C. for 5 minutes and lowered to -78.degree. C. Then 25 g (0.129 mole) of 2,4-difluoro-bromobenzene is then added and the reaction is stirred at -65.degree. C. for 2 hours. Then, 25 ml (0.164 mole) of hexachloroacetone is added and the solution is warmed at room temperature. After evaporation of the solvent, the residue is distilled under vacuum to give the desired product.
[0110] 3-Chloro-2,4-difluorobenzoic acid
[0111] To a solution of 21.5 g (0.0945 mole) of 3-chloro-2,4-difluoro-brom-obenzene in 220 ml of ether at -78.degree. C. is added 59 ml of ...
example i
COMPOSITION EXAMPLE I
[0149] A tablet composition for oral administration, according to the present invention, is made comprising:
3 Component Amount Compound of Example 12 150 mg Lactose 120 mg Maize Starch 70 mg Talc 4 mg Magnesium Stearate 1 mg
[0150] Other compounds having a structure according to Formula 1 are used with substantially similar results.
composition example ii
[0151] A capsule containing 200 mg of active for oral administration, according to the present invention, is made comprising:
4 Component Amount (% w / w) Compound of Example 13 15% Hydrous Lactose 43% Microcrystalline Cellulose 33% Crosspovidone 3.3% Magnesium Stearate 5.7%
[0152] Other compounds having a structure according to Formula 1 are used with substantially similar results.
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