本文报道了4,6-二苄基-3-氰基-2(1H)-吡啶酮的合成方法。合成了重要中间体3-氧代-4-苯基丁酸乙酯,为合成不同的6位取代的吡啶酮类化合物提供方法。对合环产物的脱羧条件进行了优化,经过甲氧基保护,以n-BuLi作为强碱,与溴苄反应得到目标化合物11。其结构经^1H NMR,^13C NMR和高分辨质谱分析确证,并对该化合物的抗HIV-1活性进行了测定。
An effective synthesis method for preparing 4,6-disubstituted pyridinones was reported. Ethyl 3-oxo-4-phenylbutyrate was an important intermediate, by which 6-substituted pyridinones could be prepared. The decarboxylation condition was optimized for compound 4. After protected with a methoxy group, the compound was reacted with BnBr to form the target compound 11. The structures were characterized by ^1H NMR, ^13C NMR and HRMS, and its enzyme inhibition activity was also determined.