【摘要】 以吡咯为起始原料,以三氟氧钒(VOF3)氧化偶联重排反应为关键步骤,经过7步反应,合成了结构骨架全新的14-羟基菲并[9,10,3’,4’]吲哚里西啶化合物8,总收率为55%.采用1HNMR,13CNMR,IR,MS和HRMS对中间体和目标产物进行了表征.初步的抗烟草花叶病毒生物活性测试结果表明,目标化合物8对烟草花叶病毒无明显抑制作用,但具有较好的抗肿瘤活性,中间体9-氧代-14-羟基-14a-甲氧基菲并[9,10,3’,4’]吲哚里西啶化合物7却表现出了很好的抗烟草花叶病毒活性.更多还原

【Abstract】 A new compound, 14-hydroxyphenanthro[9,10,3’,4’]indolizidine (8), has been synthesized utilizing pyrrole as starting material via the oxidative coupling and rearrangement reactions by vanadium oxytrifluoride (VOF3) in seven steps in an overall yield 55%. The structures of the target compound and its precursors were confirmed by 1H NMR, 13C NMR, IR, MS and HRMS techniques. Preliminary bioassay showed that 8 had weak antiviral activity against tobacco mosic virus (TMV), but exhibited potential anti- tumour activity. The intermediate 9-oxo-14-hydroxy-14a-methoxyphenanthro[9,10,3’,4’]indolizidine (7) exhibited excellent antiviral activity against TMV.更多还原