阿普斯特合成路线图解

Graphical Synthetic Routes of Apremilast

阿普斯特是美国Celgene公司研发的一种口服类的选择性磷酸二酯酶4(PDE4)抑制剂,通过调节胞内促炎与抗炎因子,抑制参与银屑病发病机制中的多个炎症的活性,从而有效治疗银屑病。阿普斯特分别获得FDA、EMA监管机构批准用于活动性银屑病关节炎和中度至重度斑块型银屑病的治疗。因此对其研究具有重要的意义。本文对阿普斯特的合成路线进行了总结,利用图解的方式对阿普斯特合成路线进行了综述和评价。

Apremilast,which was developed by Celgene Corporation Company,is the first oral inhibitor of phosphodiesterase 4.It is effective in the treatment of psoriasis by regulating intracellular pro-inflammatory and antiinflammatory factors and inhibiting the activity of multiple inflammatory factors involved in the pathogenesis of psoriasis.It has been approved by FDA and EMA for the treatment of active psoriatic arthritis(PsA)and plaque psoriasis who are candidates for phototherapy or systemic therapy.The study for its synthesis has important significance.In this article,we conclude its synthetic route,graphic method was used to review and evaluate its synthetic process.