新产品编号:1158533
Chemical Name: 4-Chloro-N-[4-[1H-imidazol-4(5)-yl]butyl]benzylsulfonamide
项目整合开发状态: Biological Testing
项目研究机构: James Black Foundation (Originator)
合成路线:The known 5-(4-chlorobutyl)-2-(tert-butyldimethylsilyl)-1-(N,N-dimethylsulfamoyl) imidazole (I) was hydrolyzed with HCl in boiling aqueous ethanol and then protected as the triphenylmethyl derivative (II) using trityl chloride and triethylamine.The required primary amine (V) was obtained by condensation of chloride (II) with potassium phthalimide (III),followed by hydrazinolysis of the resulting N-alkylated phthalimide (IV).Sulfonylation of amine (V) with 4-chlorobenzylsulfonyl chloride (VI) gave rise to the sulfonamide (VII).The trityl protecting group of (VII) was finally removed by acid treatment.
📌 参考资料/链接:
参考文献标题:Histamine H3 receptor ligands
文献作者:Kalindjian,S.B.; Shankley,N.P.; Tozer,M.J.; McDonald,I.M.; Pether,M.J.; Harper,E.A.; Watt,G.F.; Cooke,T.; Low,C.M.R.(James Black Foundation Ltd.)
参考来源:EP 0882023; JP 2000505428; US 6080871; WO 9729092