以天然橙皮素(1)为原料,经选择性甲基化和异戊烯基化半合成得到了桃皮素(2)和7-O-异戊烯基橙皮素(3).1~3分别与盐酸羟胺、盐酸甲氧胺、盐酸苄氧胺反应合成了9个E构型的橙皮素肟类化合物.所合成产物通过NMR,HR-ESI-MS方法进行了结构确证.噻唑蓝(MTT)蛋白染色法体外抑制肿瘤增值活性测试发现部分化合物对胃癌细胞SGC-7901有明显的抑制活性. Peachthrine (2) and 7-O-prenyl hesperetin (3) were obtained from natural hesperetin (1) by selective methylation and prenylation. (1) ~ 3, respectively, with hydroxylamine hydrochloride, methoxyamine, benzylamine hydrochloride synthesis of nine E-configuration of the hesperein oxime compounds were synthesized by NMR, HR-ESI-MS method was confirmed by the structure. In vitro inhibition of tumor proliferation activity by MTT staining showed that some compounds showed significant inhibitory activity on SGC-7901 gastric cancer cells.