| 吉莫斯特的合成 |
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| 引用本文： | 郝玲花,周洁,孙延龙,王友奇,曾昭钧. 吉莫斯特的合成[J]. 沈阳药科大学学报, 2005, 22(6): 420-421,433 |
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| 作者姓名： | 郝玲花 周洁 孙延龙 王友奇 曾昭钧 |
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| 作者单位： | 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 |
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| 摘 要： | 目的合成二氢嘧啶脱氢酶抑制剂吉莫斯特。方法以丙二腈、原乙酸三甲酯和1,1二甲氧基三甲胺为起始原料制备1,1二氰基2甲氧基4(N,N二甲基氨基)1,3丁二烯,经体积分数为80%的冰醋酸环合得3氰基4甲氧基2(1H)吡啶酮,再经NCS氯代形成5氯3氰基4甲氧基2(1H)吡啶酮,经质量分数为48%的HBr水解得吉莫斯特。结果合成了吉莫斯特,总收率达65.6%,各步中间体结构由MS1、H NMR确证,目标产物经MS、1H NMR以及元素分析确证。结论该工艺路线成本较低,反应条件温和,操作简便,容易实现工业化生产。
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| 关 键 词： | 吉莫斯特 抗癌药物 药物合成 |
| 文章编号： | 1006-2858（2005）06-0420-02 |
| 收稿时间： | 2005-01-14 |
| 修稿时间： | 2005-01-14 |
Studies on the synthesis of gmeracil |
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| HAO Ling-hua,ZHOU Jie,SUN Yan-long,WANG You-qi,ZENG Zhao-jun. Studies on the synthesis of gmeracil[J]. Journal of Shenyang Pharmaceutical University, 2005, 22(6): 420-421,433 |
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| Authors: | HAO Ling-hua ZHOU Jie SUN Yan-long WANG You-qi ZENG Zhao-jun |
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| Affiliation: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China;School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | Objective To synthesize gimeracil,which is a potent dihydropyrimidine dehydrogenase inhibitor.Methods Gimeracil was synthesized by four steps from malononitrile,trimethyl orthoacetate and 1,1-dimethoxy-trimethylamine via condensation,cyclization,chlorination and hydrolysis reactions.Results Gimeracil was synthesized in overall yield of 65.6%,its structure was confirmed by MS,()~1H-NMR as well as elemental analysis.Intermediate compounds were confirmed by MS and()~1H-NMR.Conclusions The improved process has advantages of lower cost,mild reaction conditions,convenient work-up.It is suitable for industrial production. |
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| Keywords: | gimeracil anticancer drug drug systhesis |
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