CNS-5161

鸟嘌呤,N'-[2-氯-5-(甲硫)苯]-N-甲基-配-[3-(甲基硫)苯]-Chemical Name: N1-[2-Chloro-5-(methylsulfanyl)phenyl]-N3-methyl-N3-[3-(methylsulfanyl)phenyl]guanidine
CAS No. 160754-76-7
项目整合开发状态: Phase II
项目研究机构: CeNeS (Originator)
合成路线:Treatment of 3-(methylsulfanyl)aniline (I) with cyanogen bromide affords the cyanamide (II),which is further N-alkylated with iodomethane and NaH to afford (III).Subsequent condensation of cyanamide (III) with 2-chloro-5-(methylsulfanyl)aniline hydrochloride (IV) in refluxing chlorobenzene gives rise to the desired guanidine derivative.
📌 参考资料/链接:
参考文献标题:Therapeutic substd.guanidines
文献作者:Durant,G.J.; Magar,S.; Hu,L.-Y.(CeNeS Pharmaceuticals)
参考来源:EP 0705100; JP 1996510754; WO 9427591

📄 详细内容


合成路线:Treatment of 3-(methylsulfanyl)aniline (I) with cyanogen bromide affords the cyanamide (II),which is further N-alkylated with iodomethane and NaH to afford (III).Subsequent condensation of cyanamide (III) with 2-chloro-5-(methylsulfanyl)aniline hydrochloride (IV) in refluxing chlorobenzene gives rise to the desired guanidine derivative.

参考文献标题:Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers
文献作者:Hu,L.-Y.; Guo,J.; Magar,S.S.; Fischer,J.B.; Burke-Howie,K.J.; Durant,G.J.
参考来源:J Med Chem 1997,40(26),4281


合成路线:The methylation of N-[3-(methylsulfanyl)phenyl]cyanamide (I) with C3H3-I and NaH in THF gives the methylated cyanamide (II),which is then condensed with 2-chloro-5-(methylsulfanyl)aniline (III) in refluxing chlorobenzene to afford the target labeled guanidine.

参考文献标题:Synthesis of N-(2-chloro-5-methylthiophenyl)-N'-(3-methyl-thiophenyl)-N'-[3H3]methylguanidine,([3H3]CNS-5161)
文献作者:Gibbs,A.R.; et al.
参考来源:J.Label.Comp.and Radiopharm.2002,45(5),395


合成路线:Treatment of 3-(methylsulfanyl)aniline (I) with cyanogen bromide affords the cyanamide (II),which is further N-alkylated with iodomethane and NaH to afford (III).Subsequent condensation of cyanamide (III) with 2-chloro-5-(methylsulfanyl)aniline hydrochloride (IV) in refluxing chlorobenzene gives rise to the desired guanidine derivative.
参考文献标题:Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands
文献作者:Dumont,F.; Sultana,A.; Waterhouse,R.N.
参考来源:Bioorg Med Chem Lett 2002,12(12),1583


产品链接: CAS No. 160754-76-7››