| 尿嘧啶还原酶抑制剂5-乙炔基尿嘧啶的合成工艺研究 |
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| 引用本文： | 李强,王尊元,马臻,沈正荣. 尿嘧啶还原酶抑制剂5-乙炔基尿嘧啶的合成工艺研究[J]. 中国药物化学杂志, 2003, 13(4): 227-229 |
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| 作者姓名： | 李强 王尊元 马臻 沈正荣 |
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| 作者单位： | 浙江省医学科学院药物研究所,浙江,杭州,310013 |
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| 基金项目： | 浙江省医药卫生研究基金资助项目 (2 0 0 2A0 0 5 ) |
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| 摘 要： | 目的 合成5-乙炔基尿嘧啶并进行工艺研究。方法 以乙酰乙酸乙酯与原甲酸三乙酯为起始原料，缩合得到α-乙氧亚甲基乙酰乙酸乙酯，再与尿素环合得到5-乙酰基尿嘧啶，之后通过氯化、水解得到尿嘧啶还原酶抑制剂5-乙炔基尿嘧啶。结果与结论 与文献报道的方法相比，该合成路线具有原料价廉易得、反应条件温和等优点。
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| 关 键 词： | 药物化学 工艺改进 化学合成 5－乙炔基尿嘧啶 尿嘧啶还原酶抑制剂 |
| 文章编号： | 1005-0108(2003)04-0227-03 |
Study on the synthetic technique of the inactivator of dihydropyrimidine dehydrogenase 5-ethynyluracil |
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| LI Qiang,WANG Zun-yuan,MA Zhen,SHEN Zheng-rong. Study on the synthetic technique of the inactivator of dihydropyrimidine dehydrogenase 5-ethynyluracil[J]. Chinese Journal of Medicinal Chemistry, 2003, 13(4): 227-229 |
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| Authors: | LI Qiang WANG Zun-yuan MA Zhen SHEN Zheng-rong |
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| Abstract: | Aim To synthesize 5-ethynyluracil,an inactivator of dihydropyrimidine dehydrogenase. Methods Ethyl acetoacetate reacted with triethyl orthorformate to give the corresponding ethoxymethylene derivative,then cyclized with urea to afford 5-acetyluracil.Chloridization of 5-acetyluracil with POCl_3 yielded 5-(1-chlorovinyl)-2,4-dichloropyrimidine,which was converted to the target compound by hydrolysis in a base solution. Results 5-ethynyluracil was successfully prepared and the synthetic route has the advantages of easy operation,low cost and being suitable for industrial production. |
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| Keywords: | medical chemistry process improvement chemical synthesis 5-ethynyluracil inactivator of dihydropyrimidine dehydrogenase |
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