PENG You,YU Guo-zhen,LANG Shao-jie,et al.Design and Synthesis of Novel Genistein Naphthylsulfonate Prodrugs[J].Soybean Science,2013,32(06):854-857.[doi:10.11861/j.issn.1000-9841.2013.06.0854]
新型大豆异黄酮萘磺酸酯前药的设计合成
- Title:
- Design and Synthesis of Novel Genistein Naphthylsulfonate Prodrugs
- Keywords:
- Soy isoflavone; Genistein; Naphthylsulfonate; Synthesis; Alkylation
- 文献标志码:
- A
- 摘要:
- ?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。
- Abstract:
- ?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 1 H NMR spectra.Synthesis of the key intermediate 2 was optimized by parallel experimental optimization method,and its alkylation reaction chemistry was analyzed preliminarily.
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备注/Memo
?国家自然科学基金(81160412);江西省自然科学基金(2010GZN0106)。