Application of composition of piperazinyl and 1H-tetrazole-based derivatives of Psiguadial A in prevention and treatment of renal fibrosis
A technology for renal fibrosis and renal interstitial fibrosis, applied in drug combinations, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as low safety and high toxicity
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Embodiment 1
[0010] Example 1 Preparation of 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 2 Psiguadial 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-(piperazinyl) ethyl derivative (III) of embodiment 3 Psiguadial A
[0020] Compound II (344mg, 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 4h. 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=100:1.0, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound III (254.8...
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