网站主页>>>项目整合精选>>>项目整合精选>>>新产品编号:1884671

新产品编号:1884671

Chemical Name: N-[1-Benzyl-5-oxopyrrolidin-2(S)-ylcarbonyl]-4-(2,6-dichlorobenzamido)-L-phenylalanine
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Coupling of N-benzylpyroglutamic acid (I) with 4-nitrophenylalanine methyl ester (II) by means of O-benzotriazolyl-N,N,N?N?tetramethyluronium hexafluorophosphate (HBTU) produced amide (III).After stannous chloride mediated reduction of the nitro group of (III),the resulting aniline (IV) was coupled with 2,6-dichlorobenzoic acid (V) to give diamide (VI).The title carboxylic acid was then obtained by ester hydrolysis with NaOH.
📌 参考资料/链接:
参考文献标题:N-Benzylpyroglutamyl-L-phenylanine derivatives as VCAM/VLA-4 antagonists
文献作者:Chen,L.; Tilley,J.W.; Guthrie,R.W.; Mennona,F.; Huang,T.N.; Kaplan,G.; Trilles,R.; Miklowski,D.; Huby,N.; Schwinge,V.; Wolitzky,B.; Rowan,K.
参考来源:Bioorg Med Chem Lett 2000,10(8),729