Composition and application thereof in antibacterial drugs
An antibacterial drug and composition technology, which can be used in antibacterial drugs, antifungal agents, and resistance to vector-borne diseases, etc., can solve problems such as difficulties in tuberculosis prevention and control, and non-standard treatment and management of tuberculosis patients.
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Embodiment 1
[0017] The preparation of embodiment 1 compound Artalbicacid
[0018] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).
[0019]
Embodiment 2
[0020] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid
[0021] Compound I (266 mg, 1.00 mmol) was dissolved in 10 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 40 °C for 16 h. After 16 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 for 5 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=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (272mg, 73%...
Embodiment 3
[0026] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Artalbicacid
[0027] Compound II (187mg, 0.5mmol) was dissolved in 15mL 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 12h . After the reaction, the reaction solution was poured into ice water, extracted 4 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=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III (111.3mg, 61% ...
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