大黄酸-N-β-羟乙基替加氟酯的合成及其骨亲和性

Synthesization of 1,8-dihydroxy-9,10-anthraquinone-2-carboxylic acid-β-(N-tegafur) hydroxy ethyl ester and its bone affinity

【目的】研究大黄酸衍生物的合成方法,探讨其骨亲和性。【方法】将大黄酸与替加氟衍生物耦联合成骨靶向的新型大黄酸衍生物,结构经质谱及核磁共振谱证实。用羟基磷灰石吸附试验评价它的体外骨亲和性。【结果】合成了大黄酸-N-β-羟乙基替加氟酯。实验显示该化合物的骨亲和性与四环素接近。【结论】大黄酸-N-β-羟乙基替加氟酯具有良好的骨亲和性。

[Objective] To study the method of synthesizing derivatives of rhein and its bone affinity. [Methods] Rhein was linked to derivative of tegafur to prepare a new derivative of bone-target compound. Its structure was identified by ^1 HNMR and MS. The compound was carried out the bone affinity assay with hydroxyapative adsorption experiment. [Results] 1,8-dihydroxy-9, 10-anthraquinone-2-carboxyhc acid-β- （N-tegafur） hydroxyethyl ester was synthesized. The result shows that the bone affinity of the compound was similer to that of tetracycline. [ Conclusions] 1,8 -dihydroxy-9,10 -anthraquinone-2-carboxylic acid-β- （N-tegafur） hydroxyethyl ester has good bone affinity.