Composition and application of composition to preparation of anti-osteoporosis medicines
An anti-osteoporosis and osteoporosis technology, applied in drug combinations, medical preparations containing active ingredients, bone diseases, etc., can solve problems such as low safety and high toxicity, and achieve prevention of osteoporosis and inhibition of osteoporosis. Mass destruction, beneficial to the effect of bone deposition
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Embodiment 1
[0014] The preparation of embodiment 1 compound SalviskinoneA
[0015] The preparation method of compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsaki et al., 2011. Salviskinone A, aditerpenewithanewskeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).
[0016]
Embodiment 2
[0017] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SalviskinoneA
[0018] Compound I (312 mg, 1.00 mmol) was dissolved in 15 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 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), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound II (327mg, 78%)...
Embodiment 3
[0023] The synthesis of the O-(imidazolyl) ethyl derivative (III) of embodiment 3SalviskinoneA
[0024] Compound II (209 mg, 0.5 mmol) was dissolved in 30 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (252 mg, 1.5 mmol) and imidazole (870 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction, the reaction solution was poured into 45 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=100:0.2, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain compound III as a light brown ...
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