Composition 55092202050677 and application thereof in drug for preventing and treating liver injury
A technology of liver damage and composition, which is applied in the field of organic synthesis and medicinal chemistry, and can solve the problems of high toxicity of liver damage, liver damage, and elevated
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Embodiment 1
[0010] The preparation of embodiment 1 compound Schiglautone A
[0011] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.
[0012]
Embodiment 2
[0013] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SchiglautoneA
[0014] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%) ...
Embodiment 3
[0019] Synthesis of O-(tetrahydropyrrolyl) ethyl derivative (III) of embodiment 3 Schiglautone A
[0020] Compound II (358 mg, 0.5 mmol) was dissolved in 15 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (168 mg, 1.0 mmol) and pyrrolidine (2840 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 6 h. After the reaction, the reaction solution was poured into ice water, extracted 4 times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III (215.8m...
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