利用前药原理对大豆异黄酮染料木素进行化学修饰,以提高染料木素的生物利用度进而改善其生物活性。结果成功设计合成了4个新型染料木素萘磺酸酯衍生物(2~5),所有新化合物的结构均经IR、MS、元素分析和1H NMR确证。采用平行实验优选法优化关键中间体2的合成,并对其烷基化反应化学进行了初步分析。 Chemical modification of soy isoflavone genistein based on the principle of prodrug to improve the bioavailability of genistein and improve its biological activity. Results Four novel genistein naphthalene sulfonate derivatives (2 ~ 5) were successfully designed and synthesized. The structures of all new compounds were confirmed by IR, MS, elemental analysis and 1H NMR. The synthesis of key intermediate 2 was optimized by the parallel experimental optimization method, and its alkylation reaction chemistry was preliminarily analyzed.