Composition and application of composition to anti-rhinitis medicine
A composition and technology for rhinitis, which are applied in the directions of drug combination, medical preparation containing active ingredients, pharmaceutical formula, etc., can solve the problems of poor curative effect and ineffectiveness of rhinitis
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Embodiment 1
[0012] The preparation of embodiment 1 compound SalviskinoneA
[0013] The preparation method of the compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsaki et al., 2011. Salviskinone A, aditerpenewithanewskeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).
[0014]
Embodiment 2
[0015] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SalviskinoneA
[0016] Compound I (312 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 12 h. After 12 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 four 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=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound II (327mg, 78%)...
Embodiment 3
[0021] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3SalviskinoneA
[0022] Compound II (210mg, 0.5mmol) was dissolved in 20mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and diethylamine (1460mg, 20mmol) were added thereto, and the mixture was heated to reflux for 8h . After the reaction, the reaction solution was poured into ice water, extracted three 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=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound III (137.7mg, ...
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