The 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoline N oxides(nitrones)(a) in anhydrous DMF was refluxed for 3-4 hours and ten of 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoles(b) were given with good yields(43%-81%) via t...The 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoline N oxides(nitrones)(a) in anhydrous DMF was refluxed for 3-4 hours and ten of 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoles(b) were given with good yields(43%-81%) via thermolysis. All of the 4 arylisoxazoles were identified with IR, \{ 1H NMR\}, \{ 13 C NMR\}, MS and elemental analysis. A novel and convenient synthetic method of 4 arylisoxazol was porvided.展开更多
文摘The 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoline N oxides(nitrones)(a) in anhydrous DMF was refluxed for 3-4 hours and ten of 4 aryl 3,5 bis(methoxycarbonyl) 2 isoxazoles(b) were given with good yields(43%-81%) via thermolysis. All of the 4 arylisoxazoles were identified with IR, \{ 1H NMR\}, \{ 13 C NMR\}, MS and elemental analysis. A novel and convenient synthetic method of 4 arylisoxazol was porvided.
文摘针对市场上的抗乙肝病毒药物存在毒副作用、耐药性等问题,为进一步研发新的抗乙肝病毒有效药物,以莽草酸为原料设计合成了22个苯异噁唑基莽草酰胺类化合物,用1H NMR、13C NMR和MS方法对化合物的结构进行表征,并对合成得到的化合物进行抗乙肝病毒体外活性实验。结果表明:苯异噁唑基莽草酰胺衍生物的毒性低,化合物11、14、15、17较好地抑制乙肝病毒HBeAg和HBsAg的分泌。活性化合物的分子对接结果显示,化合物与核心蛋白片段(PDB ID 3KXS)具有较好的相互作用。
