Pyrazoloacridine, PZA, NSC-366140, PD-115934
NSC366140无结构图 PYRAZOLOACRIDINE无结构图 Chemical Name: 9-Methoxy-N,N-dimethyl-5-nitro-2,6-dihydropyrazolo[3,4,5-kl]acridine-2-propanamine; 2-[3-(Dimethylamino)propyl]-9-methoxy-5-nitro-2,6-dihydropyrazolo[3,4,5-kl]acridine
CAS No. 99009-20-8, 99009-21-9 (methanesulfonate)
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator), National Cancer Institute (Codevelopment)
合成路线:The condensation of 4-methoxyaniline (I) with 2,6-dichloro-3-nitrobenzoic acid (II) by means of DIEA or N,N-dimethylaniline at 75 C gives 6-chloro-2-(4-methoxyphenylamino)-3-nitrobenzoic acid (III),which is cyclized in refluxing POCl3 to yield the acridone (IV).Finally,this compound is condensed with N-[3-(dimethylamino)propyl]hydrazine (V) in THF/methanol to afford the target 2,6-dihydro-pyrazolo[3,4,5-kl]acridine.
📌 参考资料/链接：
参考文献标题:Pyrazolo[3,4,5-kl]acridine cpds.,pharmaceutical compsns.the same and processes for their production
文献作者:Capps,D.B.(Pfizer Inc.)
参考来源:EP 0138302; ES 8701758; ES 8703468; ES 8703874; ES 8703875; JP 1985069084; JP 1994041127; US 4555572
📄 详细内容
合成路线:The condensation of 4-methoxyaniline (I) with 2,6-dichloro-3-nitrobenzoic acid (II) by means of DIEA or N,N-dimethylaniline at 75 C gives 6-chloro-2-(4-methoxyphenylamino)-3-nitrobenzoic acid (III),which is cyclized in refluxing POCl3 to yield the acridone (IV).Finally,this compound is condensed with N-[3-(dimethylamino)propyl]hydrazine (V) in THF/methanol to afford the target 2,6-dihydro-pyrazolo[3,4,5-kl]acridine.
参考文献标题:2-(Aminoalkyl)-5-nitropyrazolo[3,4,5-kl]acridines,a new class of anticancer agents
文献作者:Capps,D.B.; Dunbar,J.; Kesten,S.R.; Shillis,J.; Werbel,L.M.; Plowman,J.; Ward,D.L.
参考来源:J Med Chem 1992,35(26),4770
产品链接: CAS No. 99009-20-8›› 产品链接: CAS No.99009-21-9››