Isofebrifugine, as a kind of natural quinazolinone alkaloid with important physiological activities and good pharmacological effects, was isolated from a Chinese medicinal plant, Chang Shan (Dichroa febrifuga). In this paper, the synthesis of a series of novel isofebrifugine analogues was accomplished by employing the N-alkylation of 4(3H)-quinazolinones with benzyl (3aR,7aR)-rel-2- (bromomethyl)hexahydrofuro[3,2-b]pyridine-4(2H)carboxylates and the subsequent N-deprotection. These analogues were characterized by 1H NMR, 13C NMR and HRMS spectra. The MTT assay was used to examine the inhibitory effects of these analogues on the growth of human hepatoma cells (HepG2). The results indicated that some halogenated or hemiketal analogues showed interesting inhibition activity.

从中草药常山（Dichroa febrifuga）中分离得到异氟苯丙氨酸，它是一种具有重要生理活性和良好药理作用的天然喹唑啉酮生物碱。在本文中，通过使用4（3H）-喹唑啉酮与苄基（3aR，7aR）-rel-2-（溴甲基）六氢呋喃[3,2-b]的N-烷基化反应，完成了一系列新型异氟苯丙氨酸类似物的合成。 ]吡啶-4（2H）羧酸酯化，随后进行N-脱保护。这些类似物通过1 H NMR，13 C NMR和HRMS光谱进行表征。使用MTT测定法检查这些类似物对人肝癌细胞（HepG2）生长的抑制作用。结果表明，某些卤代或半缩酮类似物显示出令人感兴趣的抑制活性。