一种基于硫胺素二硫化物传递系统的5-Fu脑靶向前药的合成
Synthesis of the brain-targeted prodrug of 5-fluorouracil based on thiamine disulfide
作者：陈瑶瑶;樊维;余永国;吴勇;
Author：
收稿日期： 年卷（期）页码：2010,25(02):-123-125
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：脑靶向;前药;硫胺素二硫化物;5-氟尿嘧啶;合成
Key words：
基金项目：国家自然科学基金资助项目(批准号:30672537)
中文摘要
目的合成一种基于硫胺素二硫化物传递系统的5-氟尿嘧啶(5-Fu)脑靶向前药。方法5-Fu在六甲基二硅胺和三甲基氯硅烷的作用下生成中间体Ⅱ,Ⅱ与5-苄氧羰基戊酰氯经选择性酰化形成中间体Ⅲ,Ⅲ再脱苄,得到中间体Ⅳ,将按文献制得的中间体Ⅴ与中间体Ⅳ偶合得到目标化合物。结果和结论目标化合物及重要中间体均经IR、1HNMR、MS等确证。
英文摘要
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