QYL-972
Chemical Name: 2(S)-[2-[(Z)-2-Amino-6-methoxy-9H-purin-9-ylmethylene]cyclopropylmethoxy(phenoxy)phosphorylamino]propionic acid methyl ester; (Z)-N-[2-(2-Amino-6-methoxypurin-9-ylmethylene)cyclopropylmethoxy(phenoxy)phosphoryl]-L-alanine methyl ester
项目整合开发状态: Preclinical
项目研究机构: University of Alabama at Birmingham (Originator), Wayne State University (Originator)
合成路线:The reaction of 6-chloro-9-[2-(hydroxymethyl)cyclopropylidenemethyl]purine-2-amine (I) with methanol and K2CO3 gives of 9-[2-(hydroxymethyl)cyclopropylidenemethyl]-6-methoxypurine-2-amine (II) which is then condensed with the phosphorylated L-alanine ester (III) by means of N-methylimidazole (NMI) in pyridine/THF.The intermediate the phosphorylated L-alanine ester (III) has been obtained by condensation of L-alanine methyl ester (IV) with phenyl dichlorophosphate (V) by means of TEA in dichloromethane.
📌 参考资料/链接:
参考文献标题:Synthesis and antiviral activity of phosphoralaninate derivatives of methylenecyclopropane analogues of nucleosides
文献作者:Kern,E.R.; Qiu,Y.-L.; Ptak,R.G.; Breitenbach,J.M.; Zemlicka,J.; Drach,J.C.; Cheng,Y.-C.; Lin,J.-S.
参考来源:Antivir Res 1999,43(1),37