SB-590885的合成工艺研究

Synthetic of SB-590885

SB-590885是一种新型的三芳基咪唑类B-Raf激酶抑制剂,已报道的合成方法收率较低且操作繁琐,不适合工业化生产。本文设计了一条新的合成路线,以4-溴吡啶盐酸盐为起始原料,经偶联、脱保护、加成、氧化、环合、水解等反应得到目标化合物,产物结构经1H NMR,13C NMR和MS确证,总收率为9.53%,该方法原料便宜易得、反应条件温和、操作简单且总收率较高,是一条适合工业化生产的合成路线。

SB-590885 is a new type of triarylimidazole B-Raf kinase inhibitor.The reported synthesis method has low yield and complicated operation,which is not suitable for industrial production.In this paper,a new synthetic route was designed.4-Bromopyridine hydrochloride was used as the starting material,and the target compound was obtained through coupling,deprotection,addition,oxidation,cyclization,hydrolysis and other reactions.The structure of the product was confirmed by 1H NMR,13C NMR and MS,and the total yield was 9.53%.The method had the advantages of cheap and easily available raw materials,mild reaction conditions,simple operation and high overall yield.It was a synthetic route suitable for industrial production.