PD-157667
Chemical Name: 2-(4,4-Diphenylbutyl)-6-(perhydroazepin-1-yl)-1,2,3,4-tetrahydroisoquinolin-5-ol
项目整合开发状态: Biological Testing
项目研究机构: Neurex (Originator), Pfizer (Originator)
合成路线:Alkylation of 5-hydroxyisoquinoline (I) with bromide (II) in DMF at 80 C afforded isoquinolinium salt (III).This was reduced to tetrahydroisoquinoline (IV) by catalytic hydrogenation in the presence of Pd/C.Finally,Mannich reaction with formaldehyde and perhydroazepine (V) in THF-water at r.t.provided the target compound.
📌 参考资料/链接:
参考文献标题:Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers
文献作者:Yuen,P.; Schelkun,R.M.; Szoke,B.; Tarczy-Hornoch,K.
参考来源:Bioorg Med Chem Lett 1998,8(18),2415