Application of flavone derivative in preparation of medicine for preventing or treating acute lung injury and/or acute respiratory distress syndrome
A technology for acute respiratory distress and acute lung injury, applied in the field of pharmaceutical research and development, can solve the problems of low curative effect, suppressing pulmonary edema dosage, etc., and achieve the effect of low dosage, suppressing pulmonary edema, and reducing the generation of pulmonary effusion
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Embodiment 1
[0044] The present embodiment provides a kind of flavonoid derivative, its reaction equation and preparation method are as follows:
[0045]
[0046] Weigh 20g of scutellarein and 25g of dichlorodiphenylmethane into 400mL of diphenyl ether, heat and stir at 180°C for 30 minutes, cool to room temperature, add 2L of petroleum ether dropwise, and filter out the solid. The solid was dissolved in ethyl acetate and mixed with silica gel (dry loading), and the silica gel column was used to Purification, followed by eluting with a mixture of petroleum ether and ethyl acetate with a volume ratio of 10:1, 3:1, and 1:1, and collecting petroleum ether and ethyl acetate with a volume ratio of 3:1 according to the TLC results The eluate obtained as the eluent was concentrated and crystallized to obtain compound 1 (25.13 g, yield 79.6%) as a yellow solid.
Embodiment 2
[0048] The present embodiment provides a kind of flavonoid derivative, its reaction equation and preparation method are as follows:
[0049]
[0050] Weigh 500 mg of compound 1 prepared in Example 1, add it to 25 mL of DMF, add 260 mg of potassium carbonate, and then add 200 μl of benzyl bromide to obtain a mixture, which is stirred in an ice-water bath (0° C.) for 2 h, and left at room temperature for 12 hours. The mixture was dissolved in 150 mL of water, extracted 3 times with ethyl acetate, 80 mL each time, the collected organic layer was washed with 200 mL of saturated brine, dried over sodium sulfate, and concentrated under reduced pressure to obtain a crude solid, which was dissolved in ethyl acetate Mix the sample with silica gel (dry loading), then pass through the silica gel column Purify, using the mixed solution of petroleum ether and ethyl acetate that volume ratio is 10:1, 5:1, 2:1, 1:1 successively as eluent to carry out gradient elution, collect according t...
Embodiment 3-8
[0052] This example provides a series of flavonoid derivatives, which are all prepared by the following reaction equation and preparation method, the difference is that the raw materials H-R 3 And the consumption of this raw material is different, thereby obtains different products, specifically see the following table:
[0053] The raw material of embodiment 3-8, product and reaction yield
[0054]
[0055] Embodiment 3-8 all adopts following reaction equation and preparation method as follows:
[0056]
[0057] Weigh the corresponding raw materials H-R according to the quality in Table 1 3 , weigh 8ml of DMF (dimethylformamide) and add to 500mlCCl 4 In the solution, after stirring at room temperature for 30min, add CCl containing 120g bis(trichloromethyl)carbonate dropwise. 4 Solution 200ml. The mixture was slowly refluxed at 75°C for 6 hours, and naturally cooled to room temperature. After the reaction solution was concentrated under reduced pressure, the crude r...
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