| 1-芳基-2-吡咯烷酮化合物的硝化反应研究 |
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| 引用本文： | 周雨,王德传,梁宇楠,张慧鑫.1-芳基-2-吡咯烷酮化合物的硝化反应研究[J].精细化工中间体,2014(6):46-48. |
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| 作者姓名： | 周雨 王德传 梁宇楠 张慧鑫 |
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| 作者单位： | 中国药科大学理学院 |
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| 摘 要： | 以1-4-(乙氧羰基)苯基]-5,5-二甲酸二乙酯-2-吡咯烷酮(2)为原料,经硝化得1-4-(乙氧羰基)-2-硝基苯基]-5,5-二甲酸二乙酯-2-吡咯烷酮(1),并对硝化条件进行优化,优化的反应条件为:以8 m L乙酸酐为溶剂,投料比为n(H2SO4)∶n(KNO3)∶n(2)=6∶2∶1,反应时间为1.5 h,反应温度为0℃以下;优化条件下目标化合物的收率为78.7%。
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| 关 键 词： | 1-芳基-2-吡咯烷酮 硝化 抗流感病毒 |
Study on the Nitration of 1-Aryl-2-pyrrolidinone |
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| ZHOU Yu;WANG De-chuan;LIANG Yu-nan;ZHANG Hui-xin.Study on the Nitration of 1-Aryl-2-pyrrolidinone[J].Fine Chemical Intermediates,2014(6):46-48. |
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| Authors: | ZHOU Yu;WANG De-chuan;LIANG Yu-nan;ZHANG Hui-xin |
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| Affiliation: | ZHOU Yu;WANG De-chuan;LIANG Yu-nan;ZHANG Hui-xin;School of Science, China Pharmaceutical University; |
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| Abstract: | Diethyl-（4-（ethoxycarbonyl）-2-nitrophenyl）-5-oxopyrrolidine-2,2-dicarboxylate is a key mtermectlate for BANA-206 which is an important anti-influenza drug. A novel process was developed for the synthesis of the 5-oxopyrrolidine-2,2-dicarboxylate in 78.7% yield via nitration. The reaction conditions were obtained as the follows： the molar ratio of the reagents n（H2SO4）：n（KNO3）：n（1）=6：2：1, the reaction time is 1.5 h and the reaction temperature is below 0℃. |
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| Keywords: | pyrrolidinone nitration anti-influenza virus |
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