A class of aryl borate derivatives of 2-butynols and their applications
A technology of aryl borate and derivatives, which is applied in the field of aryl borate derivatives, can solve problems such as stimulation of the gastrointestinal tract, loss of consciousness, respiratory failure, etc., and achieve the effect of reducing side effects
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Embodiment 1
[0013] Embodiment 1: the synthesis of target compound:
[0014] 1.1 Synthesis of target compound 1:
[0015] synthetic route:
[0016]
[0017] Operation: Dissolve triphosgene (1.78g, 6mmol) in 40mL of toluene at 0°C, then slowly add pyridine (0.47g, 6mmol) in 30min and dissolve in 10mL of toluene, then (+) 2-azolium Alcohol (0.62 g, 4 mmol) was added slowly over 30 min and dissolved in 40 mL of toluene, then stirred at room temperature for 24 h. After the reaction was complete, toluene was distilled off under reduced pressure to obtain white crystals, which were dissolved in 30 mL of dichloromethane. At 0°C, 10 mL of dichloromethane and 2 mL of DMSO were dissolved in 4-hydroxymethylphenylboronic acid methyl ester (0.72 g, 4 mmol) , was added dropwise to the above solution, and triethylamine (0.4 g, 4 mmol) was added dropwise to the above reaction solution, and then stirred at room temperature for 24 h. After the reaction was completed, the white solid was removed by fil...
Embodiment 2
[0034] Example 2: Determination of Target Compound's Sensitivity to Free Radicals
[0035] Take an appropriate amount of the target compound and prepare a solution with a concentration of 0.1 mmol / L with 95% ethanol. Take 1mL and add 2mmol / LH 2 o 2 1 mL of ethanol solution, mix well, and place at 25°C for 1 hour, and measure the concentration of 2-butynol in it. Another 1 mL was added to 1 mL of distilled water, mixed evenly, and left at 25°C for 1 hour to measure the concentration of 2-butynol.
[0036] The compound involved in the embodiment of table 1 is in H 2 o 2 Concentration of released 2-butyritol in the presence (mmol / L)
[0037] compound Aqueous solution (without H 2 o 2 )
[0038] The results showed that the target compound had good stability, and under the action of free radicals, the target compound released 2-butynol rapidly. Due to the presence of a large number of free radicals in the ischemic site, the above experimental results suggest th...
Embodiment 3
[0039] Example 3: The protective effect of the target compound on focal cerebral ischemia-reperfusion
[0040] 3.1 Preparation of focal cerebral ischemia-reperfusion model
[0041] After the mice were anesthetized with 2% chloral hydrate (0.2mL / 10g, i.p.), the animals were fixed supine on the operating table, the skin was incised along the midline of the neck, the neck muscle tissue was bluntly separated, and the right common carotid artery ( CCA) and dissociate carefully; gently dissect the accompanying vagus nerve, ligate and cut off the internal and superficial branches of the external carotid artery (ECA); follow the internal carotid artery (ICA) forward, and there is a lateral branch near the base of the skull The branch artery—the pterygopalatine artery, was separated and ligated. The proximal end of the CCA was ligated with surgical thread; the distal end of the ligature was cut with ophthalmic scissors, and a section of surgical nylon thread (No. 16-17mm (mice) until...
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