Composition and application of composition in preparation of medicines for resisting rhinitis
A composition and technology for rhinitis, applied in the directions of anti-inflammatory agents, drug combinations, medical preparations containing active ingredients, etc., can solve the problems of poor efficacy and ineffectiveness of rhinitis, and achieve good anti-rhinitis effect
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Embodiment 1
[0012] The preparation of embodiment 1 compound Artalbicacid
[0013] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).
[0014]
Embodiment 2
[0015] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid
[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%...
Embodiment 3
[0021] Synthesis of O-(piperazinyl) ethyl derivative (III) of embodiment 3 Artalbicacid
[0022] Compound II (187mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 4h. After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted twice 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 light brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compoun...
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