SCH-442416
2-(2-呋喃基)-7-[3-(4-甲氧基苯基)丙基]-7H-吡唑并[4,3-e][1,2,4]噻唑并[1,5-c]嘧啶-5-胺Chemical Name: 2-(2-Furyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine
CAS No. 316173-57-6, 316173-59-8 (labeled)
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Originator)
合成路线:The condensation between 3-(4-methoxyphenyl)propyl hydrazine (I) and (ethoxymethylene)malononitrile (II) afforded the pyrazole (III),which was transformed to the corresponding imidate (IV) by refluxing in triethyl orthoformate.Reaction of imidate (IV) with 2-furoic acid hydrazide (V) provided the pyrazolopyrimidine intermediate (VI),which was thermally cyclized in diphenyl ether to the tricyclic derivative (VII).Hydrolysis of (VII) with HCl induced the pyrimidine ring opening to furnish (VIII).This was finally converted into the title compound by treatment with cyanamide in N-methylpyrrolidone.
📌 参考资料/链接:
参考文献标题:Design,radiosynthesis,and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography
文献作者:Todde,S.; Moresco,R.M.; Simonelli,P.; Baraldi,P.G.; Cacciari,B.; Spalluto,G.; Varani,K.; Monopoli,A.; Matarrese,M.; Carpinelli,A.; Magni,F.; Kienle,M.G.; Fazio,F.
参考来源:J Med Chem 2000,43(23),4359