苯并吡喃-4-酮衍生物的合成及其趋骨性探讨  

Synthesis of benzopyran-4-one derivatives and their bone-affinity

作　　者：黄文才[1] 林钢[1] 翁玲玲[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《中国药物化学杂志》2003年第1期8-11,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金资助项目 (30 0 70 883)

摘　　要：目的根据具有趋骨性的化合物的共同特征 ,设计并合成苯并吡喃 4 酮类化合物 ,检测它们的趋骨性。方法以苯并吡喃 4 酮为核心 ,设计并合成了 6个在其 3位、5位、6位有酚羟基、甲氧基、羧基、酯基、甲氧羰甲氧基等基团的衍生物 ,用羟基磷灰石吸附实验检测其趋骨性。结果所有合成的目标化合物的结构均经过IR ,1H NMR和MS确认。结论部分设计的苯并吡喃 4 酮衍生物具有比四环素更好的趋骨性。Aim To design and synthesize benzopyran-4-one derivatives according to the common structural properties of compounds which have bone affinity and test their bone affinity.Methods With benzopyran-4-one as the core,six derivatives which have hydroxy,methoxy,carboxy,methoxycarbonyl or methoxycarbonylmethoxy at C-3,C-5 or C-6 position were synthesized.The adsorption abilities of hydroxyapatite of some target compounds were tested.Results The structures of all the target compounds synthesized were confirmed by IR, 1H-NMR and MS.Conclusion Some of the benzopyran-4-one derivatives synthesized have better bone affinities compared with tetracycline.

关 键 词：苯并吡喃-4-酮衍生物 合成 趋骨性 药物化学 制备 衍生化 羧基磷灰石 

分 类 号：R914[医药卫生—药物化学]