Application of imidazolyl and dihydroxy ethylamino derivative composition of Psiguadial A to increase of leukocyte
A technology for increasing white blood cells and compositions, applied in the field of preparation and compositions, and can solve the problems of low safety and high toxicity of white blood cells
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Embodiment 1
[0010] The preparation of embodiment 1 compound Psiguadial A
[0011] The preparation method of compound Psiguadial A (I) refers to the literature published by Meng Shao et al. (Meng Shao et al., 2010.Psiguadials A and B, Two Novel Meroterpenoids with UnusualSkeletons from the Leaves of Psidium guajava.Organic Letters 12(2010)5040- 5043) method.
[0012]
Embodiment 2
[0013] The synthesis of the O-bromoethyl derivative (II) of embodiment 2Psiguadial A
[0014] Compound I (474 mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 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=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502mg, 73%) ....
Embodiment 3
[0019] The synthesis of the O-(imidazolyl) ethyl derivative (III) of embodiment 3Psiguadial A
[0020] Compound II (344 mg, 0.5 mmol) was dissolved in 25 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (168 mg, 1.0 mmol) and imidazole (3480 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 2 h. After the reaction was completed, the reaction solution was poured into 25 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=100:0.4, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of co...
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