Application of diethylamine derivatives of cleistanone in the preparation of anti-acute gout drugs
A technology for cleistanone and acute gout, which is applied in the field of preparation of cleistanone derivatives and can solve the problems of granulocytopenia, aplastic anemia and the like, and achieve the effects of inhibiting expression, improving cell activity and reducing cell apoptosis.
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Embodiment 1
[0023] Example 1 Preparation of Compound Cleistanone
[0024] The preparation method of compound Cleistanone (I) refers to the literature published by Van Trinh Thi Thanh et al. (Van Trinh Thi Thanh et al., 2011.Cleistanone: A Triterpenoid from Cleistanthus indochinensis with a New Carbon Skeleton. 4111, August2011) approach.
[0025]
Embodiment 2
[0026] Example 2 Synthesis of O-Bromoethyl Derivatives (II) of Cleistanone
[0027] Compound I (440 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.04 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 25 °C for 24 h. After 24 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, v / v), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (344 mg, 63%).
[0028] 1H NMR (500MHz, DMSO-d 6...
Embodiment 3
[0032] Example 3 Synthesis of O-(diethylamino)ethyl derivatives (III) of cleistanone Cleistanone
[0033] Compound II (273mg, 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 was completed, 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, v / v), and the light yellow concentrated elution band was collected to obtain compound III as a light yellow colloidal solid (16...
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