5-arylamino quinolyl-7,8-dione derivative and its application in preparing antibiotic medicine
A technology of arylaminoquinoline and antibacterial drugs, which is applied in the field of drugs against methicillin-resistant Staphylococcus aureus, and can solve problems such as lack of drug treatment methods
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Embodiment 1
[0016] Example 1: OX-03
[0017] Dissolve 1.45g (10mmol) of 8-hydroxyquinoline and 1.08g (10mmol) of p-methylaniline in 20ml of DMF solution, add an appropriate amount of IBX, react at room temperature (25°C-30°C) for 2h, concentrate under reduced pressure and use 20ml Ethyl acetate was extracted three times, the solvent was evaporated to dryness, and silica gel column chromatography (CH3Cl:CH3OH: 7:3) was used to obtain 0.65 g of a brownish-red solid (about 40% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.
Embodiment 2
[0018] Example 2: GX-09
[0019] 1.45g (10mmol) of 8-hydroxyquinoline and 1.24g (10mmol) of p-methoxyaniline were dissolved in 20ml of DMF solution, an appropriate amount of IBX was added, and reacted at room temperature (25°C-30°C) for 1h, concentrated under reduced pressure and used 20ml of ethyl acetate was extracted three times, the solvent was evaporated to dryness, and then silica gel column chromatography (CH3Cl:CH3OH ratio of 7:3) was used to obtain 1.4g of a brownish red solid (about 50% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.
Embodiment 3
[0020] Embodiment 3: GX-10
[0021] 1.45g (10mmol) of 8-hydroxyquinoline and 1.72g (10mmol) of p-bromoaniline were dissolved in 20ml of DMF solution, an appropriate amount of IBX was added, and the reaction was carried out at room temperature (25°C-30°C) for 6h. Ethyl ester was extracted three times, the solvent was evaporated to dryness, and silica gel column chromatography (CH3Cl:CH3OH ratio 7:3) was used to obtain 0.82 g of a brownish-red solid (about 25% yield). The structure of the product was determined by IR, MMR, MS and elemental analysis data.
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