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N1-(芳)烷氧酰基烷酰基-5-氟尿嘧啶的合成
引用本文:海俐,吴林艳,黄娟,程丽,吴勇. N1-(芳)烷氧酰基烷酰基-5-氟尿嘧啶的合成[J]. 四川大学学报(医学版), 2004, 35(4): 552-554,562
作者姓名:海俐  吴林艳  黄娟  程丽  吴勇
作者单位:四川大学华西药学院,药物化学教研室,成都,610041;四川大学华西药学院,药物化学教研室,成都,610041;四川大学华西药学院,药物化学教研室,成都,610041;四川大学华西药学院,药物化学教研室,成都,610041;四川大学华西药学院,药物化学教研室,成都,610041
基金项目:国家自然科学基金(批准号39970869)资助
摘    要:目的合成有适当脂溶性的N1-(芳)烷氧酰基取代的5-氟尿嘧啶衍生物。方法将5-氟尿嘧啶用六甲基二硅烷胺进行硅醚化,然后再与不同的二酸单苄酯酰氯反应,得目标物(Ⅰ);(Ⅰ)经氢化脱苄,得目标物(Ⅱ);随后与卤代烃发生酯化反应,得目标物(Ⅲ)。结果合成了12个5-氟尿嘧啶衍生物。结论合成的12个5-氟尿嘧啶衍生物经^1H-NMR、IR、MS所确证为实验的设计产物。

关 键 词:N1-(芳)烷氧酰基取代的5-氟尿嘧啶衍生物  合成
修稿时间:2003-09-11

Synthesis of N1-(aryl)alkyloxyacyl-5-fluorouracil Derivatives
Li Hai,Lin-yan Wu,Juan Huang,Li Cheng,Yong Wu. Synthesis of N1-(aryl)alkyloxyacyl-5-fluorouracil Derivatives[J]. Journal of Sichuan University. Medical science edition, 2004, 35(4): 552-554,562
Authors:Li Hai  Lin-yan Wu  Juan Huang  Li Cheng  Yong Wu
Affiliation:Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610061, China.
Abstract:OBJECTIVE: To synthesize N1-(aryl)alkyloxyacyl-5-fluorouracil derivatives and investigate their antitumor activities. METHODS: Title compounds (I) were prepared by 5-fluorouracil which was trimethylsilylated by hexamethyl-di-silazane, and then acylated. Hydrogenization of compounds (I) brought on compounds (II), which were esterified to produce title compounds (III) afterwards. RESULTS: Twelve title compounds were synthesized. CONCLUSION: These compounds were designed products confirmed by 1H-NMR, IR and MS spectral data.
Keywords:N_1-(aryl)alkyloxyacyl-5-fluorouracil derivatives Synthesis
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