| 5-氟脲嘧啶的β-D-半乳吡喃糖苷的合成 |
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| 引用本文： | 孙昌俊,陈再成,张以宁,王义贵,张成如.5-氟脲嘧啶的β-D-半乳吡喃糖苷的合成[J].有机化学,1992,12(3):273-277. |
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| 作者姓名： | 孙昌俊 陈再成 张以宁 王义贵 张成如 |
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| 作者单位： | 山东大学化学系，山东大学化学系，山东大学化学系，山东大学化学系，山东大学化学系 山东，济南，250100，山东，济南，250100，山东，济南，250100，山东，济南，250100，山东，济南，250100 |
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| 摘 要： | 5-氟脲嘧及其衍生物是目前临床上广泛使用的抗代谢类抗癌药物, 主要适用于消化道癌、乳腺癌、肺癌等, 但具有一定的毒性, 主要表现为骨髓抑制和胃肠道反应。我们以Koenigs-Knorr法和相转催化法合成了5-氟脲嘧啶的两种类型(-N型, -O型)的半乳吡喃糖苷。这些糖苷类化合物在体内糖苷的作用下, 有可能缓慢地分解释放出5-氟脲嘧啶, 降低其毒性, 提高抑瘤效果。
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| 关 键 词： | 氟脲嘧啶 抗癌药 吡喃糖 相转移催化 糖苷 半乳糖 山东省自然科学基金 |
Synthesis of galactopyranosides of 5-fluorouracil |
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| SUN Chang-Jun,CHEN Zai-Cheng,ZHANG Yi-Ning,WANG Yi-Gui,ZHANG Cheng-Ru.Synthesis of galactopyranosides of 5-fluorouracil[J].Chinese Journal of Organic Chemistry,1992,12(3):273-277. |
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| Authors: | SUN Chang-Jun CHEN Zai-Cheng ZHANG Yi-Ning WANG Yi-Gui ZHANG Cheng-Ru |
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| Institution: | SUN Chang-Jun,CHEN Zai-Cheng,ZHANG Yi-Ning,WANG Yi-Gui,ZHANG Cheng-Ru Department of chemistry,Shandong University,250100 Jinan,Shandong |
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| Abstract: | Two acetyl galactopyranosides 2-O-benzyl-4-O-(2',3',4',6'-tetra-O-acetyl-b-D-galactopyranosyl)-5-fluoro uracil (I) and 2-O-benzyl-3-N-(2',3',4',6'-tetra-O-acetyl-b-D-galactopyranosyl)-5-fluoro uracil (II) were synthesized by the reaction of 2-O-benzyl-5-fluorouracil and a-acetobromogalactose (III). Under phase transfer catalysis I was also synthesized by the reaction of silver salt of 2-O-benzyl-5-fluorouracil and III. I and II were treated with ammonia in MeOH to obtain deacetylated galactopyranosides, which were hydrogenated in the presence of 10% Pd-C catalyst to obtain galactopyranosides of 5-fluorouracil, IV and V resp. |
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| Keywords: | 5-fluorouracil synthesis galactopyranoside phase transfer catalysis |
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