1, 3, 4-oxadiazole-norfloxacin heterozygote and preparation method and application thereof
A technology of norfloxacin and hybrid, which is applied in the field of antibacterial drugs, 1,3,4-oxadiazole-norfloxacin hybrid and its preparation, and can solve the problems of increased bacterial resistance
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Embodiment 1
[0023]1-ethyl-6-fluoro-7- (4 - (5- (furan-2-yl) -1,3,4-oxazole-2-yl) methyl) piperazine-1-yl Preparation of -4-oxy-1,4-dihydroquinoline-3-carboxylic acid (IIA):
[0024]
[0025]8.0 mmol of furan-2-formyl hydrazide, 9.6 mmol chloroacetyl chloride, 30 ml of ethyl acetate was added to 100 ml of flask, and the reaction was stirred at room temperature for 3 hours, and the reaction was completed, filtered, air dried to obtain a precursor compound. 4.8 mmol of precursor compound, 9.4 mmol of trichlorophos, 20 ml acetonitrile was added to 100 ml of flask, and the reaction was stirred at 70 ° C for 20 hours, the reaction was completed, and the reaction was concentrated to remove acetonitrile, and 25 ml of ethyl acetate is dissolved, and the equivalence is sequentially used. Water, saturated sodium hydrogencarbonate solution, saturated sodium chloride solution, dry dry after drying with anhydrous sodium sulfate, dried under reduced pressure to give intermediate IA, ie 2- (chloromethyll) -5- (furan...
Embodiment 2
[0028]1-ethyl-6-fluoro-7- (4 - (5- (3-hydroxyphenyl) -1,3,4-oxazole-2-yl) methyl) piperazine-1-yl Preparation of -4-oxy-1,4-dihydroquinoline-3-carboxylic acid (IIB):
[0029]
[0030]8.0 mmol of 3-hydroxybenzide hydroxyl hydrolyzide, 9.6 mmol chloroacetyl chloride, 30 ml of ethyl acetate, 100 ml of a flask, stirred at room temperature for 3 hours, completed, filtered, air dried to obtain a precursor compound. 4.8 mmol of precursor compound, 9.4 mmol of trichlorophos, 20 ml acetonitrile was added to 100 ml of flask, and the reaction was stirred at 70 ° C for 12 hours, the reaction was completed, and the reaction was concentrated to remove acetonitrile, and 25 ml of ethyl acetate is dissolved, and the equivalents were sequentially used. Water, saturated sodium hydrogencarbonate solution, saturated sodium chloride solution extraction, after drying with anhydrous sodium sulfate, dry dry, to give intermediate Ib, i.e., 3- (5- (5- (meth) -1, 3,4-oxazole-2-yl) phenol.
[0031]1.0 mmol of intermedia...
Embodiment 3
[0033]1-ethyl-6-fluoro-7- (4 - (5- (4-hydroxyphenyl) -1,3,4-oxazole-2-yl) methyl) piperazine-1-yl Preparation of -4-oxy-1,4-dihydroquinoline-3-carboxylic acid (IIC):
[0034]
[0035]8.0 mmol of 4-hydroxybenzide hydrolyzide, 9.6 mmol chloroacetyl chloride, 30 ml of ethyl acetate was added to 100 mL of flask, and the reaction was stirred at room temperature for 3 hours, and the reaction was completed, filtered, air dried to obtain a precursor compound. 4.8 mmol of precursor compound, 9.4 mmol of trichlorophos, 20 ml acetonitrile was added to 100 ml of flask, and the reaction was stirred at 70 ° C for 20 hours, the reaction was completed, and the reaction was concentrated to remove acetonitrile. Water, saturated sodium hydrogencarbonate solution, saturated sodium chloride solution, after drying with anhydrous sodium sulfate, dry drying, to give intermediate IC, i.e., 4- (5- (meth) -1, 3,4-oxazole-2-yl) phenol.
[0036]1.0 mmol of intermediate IC 4- (5- (chloromethyl) -1,3,4-malodonazole-2-yl) ...
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