L-leucine derivatives blocking entrance of H5N1 avian influenza virus and preparation method for same
A kind of derivative, technology of leucine, applied in the field of L-leucine derivative and preparation thereof
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Embodiment 13
[0034] Synthesis of embodiment 13,4-dihydroxybenzoylleucine methyl ester
[0035] Take 1.00g (6.494×10 -3 mol) 3,4-dihydroxybenzoic acid was dissolved in 10ml of anhydrous dichloromethane in a 100ml three-necked flask. Another 2.50g (1.300×10 -2 mol) ethyl-(3-dimethylaminopropyl) carbodiimide (EDCI) and 1.750g (1.300×10 -2 mol) 1-hydroxybenzotriazole (HOBT) in 10ml dichloromethane solution, and added to the above-mentioned 100ml three-necked bottle, drop 1.8ml (1300×10 -2 mol) triethylamine solution, the reaction temperature was controlled at 0°C, and the reaction was stirred for about half an hour.
[0036] Take L-leucine methyl ester hydrochloride 3g (1.65×10 -2 mol) in 30ml of anhydrous dichloromethane, add dropwise 2.3ml (1.65×10 -2 mol) triethylamine solution and suction filtered. The filtrate L-leucine methyl ester dichloromethane solution was added to the reaction flask, and the temperature was slowly raised to 30° C. for 6 hours.
[0037]After the reaction was c...
Embodiment 23
[0038] Example 23,4-Dihydroxyphenylacetylleucine methyl ester
[0039] The preparation method of step 13,4-dimethoxyphenylacetic acid methyl ester
[0040] Take 3g (17.856×10 -3 mol) 3,4-dihydroxyphenylacetic acid solid in a 100ml three-necked flask, dissolved in 50ml anhydrous acetone, and added 10.8g (7.815×10 -2 mol) potassium carbonate solid. Another 7.5ml (77.328×10 -3 mol) dimethyl sulfate solution was diluted with anhydrous acetone, which was slowly dropped into a three-necked flask and heated to reflux for 6 hours. Potassium carbonate particles were removed by suction filtration, and the solvent was distilled off, the residue was dissolved in ethyl acetate, the ethyl acetate layer was washed three times with saturated saline solution, and the ethyl acetate solution was dried over anhydrous sodium sulfate. Sodium sulfate was removed by filtration, and the ethyl acetate extract was concentrated and applied to a silica gel column, with ethyl acetate:petroleum ether (1...
Embodiment 3
[0048] Embodiment 3L-leucine derivative anti-avian influenza virus H 5 N 1 active
[0049] 1. Experimental materials
[0050] (1) Virus: H 5 N 1 The virus strain is Influenza strain A / VietNam / 1194 / 2004, and its titer was 5×10 9 PFU / ml, diluted with culture medium during infection, namely 80PFU / well, provided by the State Key Laboratory of Virology, Wuhan University.
[0051] (2) Cells: MDCK cells (sourced from China Center for Type Culture Collection, MDCK cells are classic cells for influenza virus plaque experiments), provided by the State Key Laboratory of Virology, Wuhan University.
[0052] (3) Positive control drug: amantadine, provided by the State Key Laboratory of Virology, Wuhan University.
[0053] (4) Sample treatment: Amantadine and the compound of the present invention were formulated with DMSO to make a 10 mg / ml mother solution, and diluted with DMSO to form a corresponding gradient when used.
[0054] 2. Experimental method
[0055] 2.1 Cytotoxicity tes...
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