1-芳基-2-吡咯烷酮化合物的硝化反应研究

Study on the Nitration of 1-Aryl-2-pyrrolidinone

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%。

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℃.