Synthesis method of brexpiprazole intermediate

The invention belongs to the technical field of medicines, and particularly relates to a brexpiprazole intermediate synthesis method, which comprises the following steps: mixing 4-halogenated benzothiophene, piperazine, L-hydroxyproline, cuprous oxide, carbonate and N-methyl-pyrrolidone, heating to...

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Hauptverfasser: ZHU JUNLING, YANG YAO, ZOU JIANG, PENG ZEGEN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the technical field of medicines, and particularly relates to a brexpiprazole intermediate synthesis method, which comprises the following steps: mixing 4-halogenated benzothiophene, piperazine, L-hydroxyproline, cuprous oxide, carbonate and N-methyl-pyrrolidone, heating to react under a protective atmosphere to obtain 4-piperazinyl benzothiophene, and reacting under a protective atmosphere to obtain the brexpiprazole intermediate. The yield and the purity of the brexpiprazole intermediate can be effectively improved. 本发明属于一种医药技术领域,具体是涉及一种依匹哌唑中间体的合成方法,将4-卤代苯并噻吩、哌嗪、L-羟基脯氨酸、氧化亚铜、碳酸盐和N-甲基-吡咯烷酮混合,在保护气氛下,加热反应,得到4-哌嗪基苯并噻吩,本发明可以有效提高依匹哌唑中间体的收率和纯度。