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)=...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%。展开更多
(S)-1-Allyl-2-aminomethylpyrrolidine, a key intermediate of a novel dopamine D2-receptor PET imagingagent 18F-fallypride was prepared from L-prolinamide by allylation and reduction in an overall yield of 50%.
文摘以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%。
文摘(S)-1-Allyl-2-aminomethylpyrrolidine, a key intermediate of a novel dopamine D2-receptor PET imagingagent 18F-fallypride was prepared from L-prolinamide by allylation and reduction in an overall yield of 50%.