Composition of artalbic acid derivatives in preparation of anti-rhinitis medicines
A technology for composition and rhinitis, applied in the direction of drug combination, medical preparations containing active ingredients, pharmaceutical formulas, 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 Artalbic acid
[0013] The preparation method of compound Artalbic acid (I) refers to the literature published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbic acid, a sesquiterpene with an unusual skeleton from Artemisia alba (Asteraceae) from Sicily. Tetrahedron Letters, 52 (2011) 4543–4545) approach.
[0014]
Embodiment 2
[0015] Synthesis of O-bromoethyl derivative (II) of embodiment 2 Artalbic acid
[0016] Compound I (266 mg, 1.00 mmol) was dissolved in 10 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 40 °C for 16 h. After 16 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 for 5 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 (272mg, 73%) .
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Embodiment 3
[0021] The synthesis of the O-(dichloroethylamino) ethyl derivative (III) of embodiment 3 Artalbic acid
[0022] 1. Synthesis of O-(dihydroxyethylamino)ethyl derivatives of Artalbic acid
[0023] Compound II (187 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (252 mg, 1.5 mmol) and diethanolamine (1051 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 1 h. After the reaction was completed, the reaction solution was poured into 20 mL of 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), and the ...
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