新产品编号:441887
Chemical Name: 6-[N-(3,4-Dimethoxyphenyl)-N-methylamino]pyrido[3,2-d]pyrimidine-2,4-diamine
CAS No. 216167-24-7
项目整合开发状态: Biological Testing
项目研究机构: Duquesne University (Originator), Indiana University (Originator)
合成路线:2,6-Dichloropyridine (I) was nitrated with HNO3 and H2SO4 to give nitropyridine (II).Substitution of the 2-chloro atom of (II) with cuprous cyanide at 180 C afforded nitrile (III).The remaining 6-chloro atom of (III) was then substituted with N-methyl-3,4-dimethoxyaniline (IV) in monoethyl glycol in the presence of pyridine to provide diaryl amine (V).The nitro group of (V) was further reduced with iron powder and HCl yielding the 3-amino derivative (VI).Finally,cyclization of (VI) with chloroformamidine hydrochloride (VII) in dimethylsulfone at 140 C produced the target pyridopyrimidine.
📌 参考资料/链接:
参考文献标题:6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver,Pneumocystis carinii,and Toxoplasma gondii and as antitumor agents
文献作者:Gangjee,A.; Zhu,Y.; Queener,S.F.
参考来源:J Med Chem 1998,41(23),4533