新产品编号:136561
Chemical Name: N-(3-Carboxypropanoyl)-L-valyl-N-[1(S)-(diphenoxyphosphinyl)-2-phenylethyl]-L-prolinamide
CAS No. 174391-80-1
项目整合开发状态: Preclinical
项目研究机构: Dyax (Originator), Osaka Medical College (Originator)
合成路线:Coupling of PhCH2OOC-Pro-OH (I) with diphenyl (1-amino-2-phenylethyl)phosphonate (II) by means of DCC in THF affords derivative (III),which is then subjected to hydrogenation followed by coupling with PhCH2OOC -Val-OH (IV) by means of DCC to provide peptide derivative (V).Finally,reaction of (V) with succinic anhydride in EtOAc under an atmosphere of H2 in the presence of Pd/C provides the target compound.
📌 参考资料/链接：
参考文献标题:Basic alpha-aminoalkylphosphonate derivs.
文献作者:Powers,J.C.; Ni,L.; Jackson,D.S.(Georgia Technology Research Corp.)
参考来源:US 5952307
📄 详细内容
合成路线:Coupling of PhCH2OOC-Pro-OH (I) with diphenyl (1-amino-2-phenylethyl)phosphonate (II) by means of DCC in THF affords derivative (III),which is then subjected to hydrogenation followed by coupling with PhCH2OOC -Val-OH (IV) by means of DCC to provide peptide derivative (V).Finally,reaction of (V) with succinic anhydride in EtOAc under an atmosphere of H2 in the presence of Pd/C provides the target compound.
参考文献标题:Irreversible inhibition of serine proteases by peptide derivatives of (alpha-aminoalkyl)phosphonate diphenyl esters
文献作者:Oleksyszym,J.; Powers,J.C.
参考来源:Biochemistry 1991,30(2),485