新型大豆异黄酮萘磺酸酯前药的设计合成

Design and Synthesis of Novel Genistein Naphthylsulfonate Prodrugs

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。

To improve bioavailability and biological activity of genistein, we designed and synthesized the new soy isoflavone genistein derivatives （ 2 - 5 ） according to principles of prodrugs. Their structures were characterized by IR, MS, elemental analysis and ^1H NMR spectra. Synthesis of the key intermediate 2 was optimized by parallel experimental optimization method, and its alkylation reaction chemistry was analyzed preliminarily.