封丛鹏

    摘 要 依匹哌唑是一种多巴胺和5-羟色胺活性调节剂，非典型抗精神病药物，可作为辅助药物用于重度抑郁症的辅助治疗，也可以用于成人精神分裂症的治疗。本文对依匹哌唑及其关键中间体的合成方法作了详细阐述，并评估了依匹哌唑关键中间体7-羟基喹啉-(1H)-2-酮和4-(1-哌嗪基)苯并[b]噻吩的相关合成工艺，为依匹哌唑的合成及工业化生产提供借鉴。

    关键词 依匹哌唑 7-羟基喹啉-(1H)-2-酮 4-(1-哌嗪基)苯并[b]噻吩

    中图分类号：O626.12； O626.323 文献标志码：A 文章编号：1006-1533(2021)17-0070-06

    Progress in the synthesis of brexpiprazole and its key intermediates

    FENG Congpeng

    (Shanghai Aoqi Pharmaceutical Technology Co.， Ltd.， Shanghai 200131， China)

    ABSTRACT Brexpiprazole， that may be a dopamine and 5-hydroxytryptamine activity regulator and atypical antipsychotics， can be used as adjuvant drugs in the adjuvant treatment of severe depression and can also be used in the treatment of adult schizophrenia. In this article， the synthetic routes of brexpiprazole and its key intermediates are described in detail. The related synthetic processes of 7-hydroxyquinoline -(1H) -2-one and 4-(1-piperazinyl)benzo[b]thiophene are evaluated， hopefully to provide reference for the synthesis of brexpiprazole and its industrial application. ......