苯并吡喃酮酯衍生物的合成及其趋骨性初探

Synthesis of benzopyrone ester derivatives and their bone-affinity

目的 设计并合成苯并吡喃酮酯衍生物并探索其趋骨性。方法 以 3-乙酰基 - 4 -羟基苯甲酸甲酯为原料 ,经酯化、分子内酰化、环合反应得目标物 ,并用羟基磷灰石吸附实验检测目标物的趋骨性。结果 合成的目标化物 (2a ,2b ,2c)的结构均经IR ,1HNMR ,MS及EA确认。结论 目标物 (2c)具有比四环素更强的趋骨性。

OBJECTIVE To design and synthesize benzopyrone ester derivatives and to test their bone affinity.METHODS The target compounds were synthesized from 3-acyl-4-hydroxylbenzoic acid by esterfication,intramolecular acylation and cylization.The adsorption abilities of hydroxyapatite of the target compounds were tested.RESULTS The structures of all the target compounds (2a,2b,2c) were confirmed by IR, 1H NMR,MS and EA.CONCLUSION The target compound (2c) has better bone affinities compared with tetracycline.