Application of Daphmalenine A ramification to preparing rhinitis-resisting medicine
A technology for derivatives and rhinitis, applied in the field of preparation, Daphmalenine A derivatives, can solve the problems of poor curative effect and ineffectiveness of rhinitis, and achieve good anti-rhinitis effect
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Embodiment 1
[0019] The preparation of embodiment 1 compound Daphmalenine A
[0020] The preparation method of compound Daphmalenine A (I) refers to the literature published by Yu Zhang et al. , 4103–4107) approach.
[0021]
Embodiment 2
[0022] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Daphmalenine A
[0023] Compound I (419 mg, 1.00 mmol) was dissolved in 10 mL of benzene, 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 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), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (320 mg, 61%).
[0024] 1H NMR (500MHz,...
Embodiment 3
[0028] The synthesis of the O-(tetrahydropyrrolyl) ethyl derivative (III) of embodiment 3 Daphmalenine A
[0029] Compound II (263 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and pyrrolidine (2840 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 12 h. After the reaction, the reaction solution was poured into ice water, extracted four 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), and the brown concentrated elution band was collected to obtain the O-(tetrahydropyrrolyl)ethyl derivative of Daphmale...
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