新产品编号:2278589
Chemical Name: N-[2-(N-tert-Butylcarbamoylsulfanyl)benzoyl]-beta-alaninamide
项目整合开发状态: Biological Testing
项目研究机构: Achillion (Originator), National Institutes of Health (Originator), Southern Research Institute (Originator)
合成路线:2,2'-Dithiosalicylic acid (I) is activated as the bis-succinimidyl ester (II) upon treatment with N-hydroxysuccinimide and DIC.Coupling of the active ester (II) with 3-aminopropionamide (III) gives rise to the corresponding dithiosalicylamide (IV).Reductive cleavage of the disulfide bond of (IV) using tris(2-carboxyethyl)phosphine (TCEP) affords thiol (V).The desired thiolcarbamate is then obtained by condensation of (V) with tert-butyl isocyanate in DMF.
📌 参考资料/链接:
参考文献标题:Benzamide-based thiocarbamates: A new class of HIV-1 NCp7 inhibitors
文献作者:Goel,A.; Mazur,S.J.; Fattah,R.J.; Hartman,T.L.; Turpin,J.A.; Huang,M.; Rice,W.G.; Appella,E.; Inman,J.K.
参考来源:Bioorg Med Chem Lett 2002,12(5),767