TU-572

Chemical Name: 5-Isopropoxy-2-[4-(methylsulfanyl)pyridin-2-ylmethylsulfinyl]-1H-benzimidazole
CAS No. 326592-39-6
项目整合开发状态: Preclinical
项目研究机构: Inst. Physical Chemical Res. (RIKEN) (Originator), Taisho (Originator)
合成路线:Acid hydrolysis of acetanilide (I) provided nitro aniline (II),which was further reduced to diamine (III) by catalytic hydrogenation over Pd/C.The 2-mercapto benzimidazole (IV) was then synthesized by condensation of phenylenediamine (III) with potassium ethyl xanthate.Alkylation of (IV) with the chloromethyl pyridine (V) produced the corresponding thioether adduct (VI).Finally,selective oxidation of the benzimidazolyl sulfur atom of (I) using m-chloroperbenzoic acid gave rise to the title sulfoxide.
📌 参考资料/链接:
参考文献标题:Synthesis and characterization of a potent selective protein tyrosine phosphatase inhibitor,2-[(4-methylthiopyridin-2-yl)methylsulfinyl]benzimidazole
文献作者:Hamaguchi,T.; Takahisha,A.; Kagamizono,T.; Manaka,A.; Sato,M.; Osada,H.
参考来源:Bioorg Med Chem Lett 2000,10(23),2657