阿卡他定关键中间体的合成研究

Study on Synthesis of Alcaftadine Key Intermediate

以5H-咪唑并[2,1-b]苯并吖庚因酮和N-甲基-4-哌啶酮为起始原料,经Mc Murry偶联反应得到阿卡他定的关键中间体11-(1-甲基-4-哌啶亚基)-6,11-二氢-5H-咪唑并[2,1-b]苯并吖庚因,含量95.0%,收率80.0%,其结构经MS、1H NMR、13C NMR确认。

Starting from 5H-benzo[d]imidazo[2,1-b]azepin-11 （6H）-one and N-methylpiperidin-4-one, the key intermediate of aleaftadine was synthesized by MeMurry coupling reaction. The yield of the reaction was 80%. The structure was characterized by MS, 1H NMR and 13C NMR.