新产品编号:1522393
Chemical Name: N-[6-Methyl-1-(3-methylbutyl)piperidin-2-ylcarbonyl]-4-O-(benzyl)-L-tyrosine tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Elan (Originator), Pfizer (Originator)
合成路线:Hydrogenation of 6-methylpyridine-2-carboxylic acid (I) over Pd/C in aqueous ammonia afforded the corresponding piperidine (II).Subsequent condensation of (II) with isovaleraldehyde (III),followed by catalytic hydrogenation with Pd/C provided the N-isopentyl piperidine (IV),which was finally coupled with O-benzyltyrosine tert-butyl ester (V) in the presence of benzotriazolyl tetramethyluronium hexafluorophosphate (HBTU) to furnish the target amide.
📌 参考资料/链接：
参考文献标题:Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers
文献作者:Hu,L.Y.; Ryder,T.R.; Nikam,S.S.; Millerman,E.; Szoke,B.G.; Rafferty,M.F.
参考来源:Bioorg Med Chem Lett 1999,9(8),1121
📄 详细内容
合成路线:Hydrogenation of 6-methylpyridine-2-carboxylic acid (I) over Pd/C in aqueous ammonia afforded the corresponding piperidine (II).Subsequent condensation of (II) with isovaleraldehyde (III),followed by catalytic hydrogenation with Pd/C provided the N-isopentyl piperidine (IV),which was finally coupled with O-benzyltyrosine tert-butyl ester (V) in the presence of benzotriazolyl tetramethyluronium hexafluorophosphate (HBTU) to furnish the target amide.
参考文献标题:PD 151307 analogs: Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers
文献作者:Hu,L.-Y.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1999,Abst MEDI 119