Composition and application thereof in antibacterial agents
A technology of antibacterial drugs and compositions, applied in the direction of antibacterial drugs, antifungal agents, active ingredients of heterocyclic compounds, etc., which can solve problems such as difficulties in tuberculosis prevention and treatment, and non-standard treatment and management of tuberculosis patients
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Embodiment 1
[0018] The preparation of embodiment 1 compound SalviskinoneA
[0019] The preparation method of the 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).
[0020]
Embodiment 2
[0021] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SalviskinoneA
[0022] 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
[0027] The synthesis of the O-(piperazinyl) ethyl derivative (III) of embodiment 3SalviskinoneA
[0028] Compound II (209mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 6h. After the reaction, 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=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain compound III as a light brown solid (15...
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