摘要
目的：设计并合成骨靶向雌激素弹头。方法：采用了相转移烃化、均相烃化等手段。结果：设计井合成了雌激素三位以聚乙二醇为桥与4种不同哌嗪环相连的20个衍生物，包括中间体共合成了28个化合物，全部目标物及其中3个中间体未见文献报道。新化合物结构经MS，1H—NMR，(13)C—NMR，IR和元素分析确定；结论：所合成的20个目标物可用于进一步合成骨靶向雌激素。
Objectives:to synthesized the mediates for the synthesis of bone-targetedestrogen. Methods: the methods sush as phase transfer catalyticalkylation, homogeneous phasealkylation were used. Results: twenty of estrogen derivatives that estrone or estradiol was linkedrespectively to 1, 4-piperazine-2-carboxylic acid methyl ester, 2 ketopiperazine, 3-oxo-1,4piperazine-2-acetic acid ethyl ester and 2, 5-piperazinedione through polyglycol were designed,twenty eight of compounds and three of mediates are new compounds. The structures of newcompounds were confirmed with MS, 1H-NMR, 13C-NMR, IR and element analysis. Conclusion: thetarget compounds synthesized can be used for the synthesis of bone-targeted estrogen.
出处
《武警后勤学院学报（医学版）》
CAS
1999年第1期10-17,共8页
Journal of Logistics University of PAP（Medical Sciences）
基金
国家自然科学基金!39430120
关键词
雌激素
哌嗪
合成
骨靶向
estrogen
piperazines
synthesis
bone-targeted
