Synthesis method of key raw material 2-chloro-6-methylaniline of dasatinib

The invention discloses a synthetic method of a key raw material 2-chloro-6-methylaniline of dasatinib. The method comprises the following steps: firstly, protecting a 1-site amino group of 2-nitro-6-methylaniline, then reducing a 2-site nitro group of 2-nitro-6-methylaniline into an amino group, th...

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Hauptverfasser: WANG LEI, ZHU YISHENG, LYU HONGCHAO, ZHANG JIZHE
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthetic method of a key raw material 2-chloro-6-methylaniline of dasatinib. The method comprises the following steps: firstly, protecting a 1-site amino group of 2-nitro-6-methylaniline, then reducing a 2-site nitro group of 2-nitro-6-methylaniline into an amino group, then carrying out diazotization reaction, carrying out chlorine substitution on the 2-site amino group by using cuprous chloride, and finally, carrying out acidolysis to remove a 1-site amino protecting group to obtain 2-chlorine-6-methylaniline. The method has the advantages of cheap and easily available raw materials, easily controllable reaction, simple operation steps, simple post-treatment, recyclable solvents, small pollution, and suitableness for large-scale production of generative enterprises. 本发明公开了一种达沙替尼关键原料2-氯-6-甲基苯胺的合成方法。该方法首先对2-硝基-6-甲基苯胺的1位氨基进行保护,再将其2位硝基还原为氨基,然后通过重氮化反应并以氯化亚铜进行氯取代2位氨基,最后经酸解脱去1位的氨基保护基得到2-氯-6-甲基苯胺。该方法的原料便宜易得,反应易于控制,操作步骤简单,后处理简单,所用溶剂均可回收套用,污染小,较适合生成型企业的放大生产。