3-1',1'-双膦酸乙基-5-氟尿嘧啶的合成及其初步的骨靶向性研究  

Synthesis of 3-1',1'-ethylbisphosphonates-5-fluorouracil and preliminary test for its bone targeting ability

作　　者：陈慧[1] 吴林艳[1] 曾建成[2] 吴勇[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学华西医院,四川成都610041

出　　处：《华西药学杂志》2005年第1期10-12,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目 (批准号 :3 9970 869;3 0 2 0 0 2 86)

摘　　要：目的　合成骨靶向性好的3-1 ,1 -双膦酸乙基-5-氟尿嘧啶。方法　将呋喃啶与亚乙烯基偕二膦酸四乙酯偶联,随后脱去偕二膦酸的酯基得到目标化合物,并采用羟磷灰石晶体吸附实验考察目标物的骨靶向性。结果和结论　合成了目标化合物物4,并经1ＨＮＭＲ、ＩＲ和ＭＳ确证结构;体外骨靶向性实验结果显示目标物4有较好的骨靶向性。OBJECTIVE To synthesize 3-1',1'-ethylbisphosphonates-5-fluorouracil which may have good bone targeting ability. METHODS The title compound was synthesized by coupling 1-2'-tetrahydrofurfuryl-5-fluorouracil with Tetraethyl ethylidene bisphosphonate and then the ester groups were hydrolyed specifically. Its bone targeting ability was evaluated by hydroxyapatite adhesion tests. RESULTS and CONCLUSION Title compound was confirmed by IR, 1HNMR and MS. It showed good bone targeting ability via hydroxyapatite adhesion tests.

关 键 词：靶向性 5-氟尿嘧啶 成骨 体外 羟磷灰石 MS IR 乙基 合成 乙酯 

分 类 号：R730[医药卫生—肿瘤] TQ352.1[医药卫生—临床医学]