【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%。更多还原

【Abstract】 Diethyl-(4-(ethoxycarbonyl)-2-nitrophenyl)-5-oxopyrrolidine-2,2-dicarboxylate is a key intermediate for BANA-206 which is an important anti-influenza drug. A novel process was developed for the synthesis of the title compound starting from diethyl-(4-(ethoxycarbonyl)phenyl)-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 ℃.更多还原