Synthesis method of lisethopram intermediate and lisethopram intermediate

The invention discloses a synthesis method of a key intermediate of lisethopram, which comprises the following steps: carrying out coupling reaction on a compound shown in a formula I and a compound shown in a formula II to generate a novel compound shown in a formula III, and carrying out ring clos...

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Hauptverfasser: DONG JINFU, FANG WUHONG, XIE XIAOQIANG, CHU DINGJUN, FANG JIE, GUO WANCHENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthesis method of a key intermediate of lisethopram, which comprises the following steps: carrying out coupling reaction on a compound shown in a formula I and a compound shown in a formula II to generate a novel compound shown in a formula III, and carrying out ring closing to generate a compound shown in a formula V after addition of the compound shown in the formula III and a compound shown in a formula IV. The synthesis method of the lisethopram intermediate, namely the compound shown in the formula V is simple, the lisethopram intermediate can be obtained only through two steps from the starting raw material of the compound shown in the formula I, and the intermediate obtained through the method is stable, convenient for impurity research and quality control, low in material cost and suitable for industrial production. # imgabs0 # 本发明公开了一种利司扑兰关键中间体的合成方法,包括使式I化合物与式II化合物进行偶联反应,生成新颖的式III化合物,式III化合物与式IV化合物加成后,关环生成式V化合物。本发明的利司扑兰中间体即式V化合物的合成方法简单,从起始原料式I化合物开始,只需要2步,即可得到,且本发明的方法得到的中间体