Aptiganel, CNS-1102, Cerestat(former Brand Name)
1-(3-乙基苯基)-1-甲基-2-萘-1-基胍Chemical Name: N1-(3-Ethylphenyl)-N1-methyl-N3-(1-naphthyl)guanidine
CAS No. 137159-92-3, 137160-11-3 (monoHCl)
项目整合开发状态: Discontinued
项目研究机构: CeNeS (Originator)
合成路线:(3-Ethylphenyl)cyanamide (III) was prepared by treatment of m-ethylaniline (I) with cyanogen bromide (II) in Et2O.Alkylation of (III) with iodomethane and NaH provided the N-methyl cyanamide (IV).This was finally condensed with 1-naphthylamine hydrochloride (V) by heating at 160 C or in the presence of AlCl3 as the catalyst.
📌 参考资料/链接：
参考文献标题:Tri- and tetra-substd.guanidines and their use as excitatory amino acid antagonists
文献作者:Weber,E.; Keana,J.F.W.(University of Oregon)
参考来源:JP 2002020361; US 5262568; WO 9112797
📄 详细内容
合成路线:(3-Ethylphenyl)cyanamide (III) was prepared by treatment of m-ethylaniline (I) with cyanogen bromide (II) in Et2O.Alkylation of (III) with iodomethane and NaH provided the N-methyl cyanamide (IV).This was finally condensed with 1-naphthylamine hydrochloride (V) by heating at 160 C or in the presence of AlCl3 as the catalyst.
参考文献标题:Preparation of substd.guanidines
文献作者:Durant,G.J.; Nagar,S.S.(CeNeS Pharmaceuticals)
参考来源:WO 9319042
合成路线:(3-Ethylphenyl)cyanamide (III) was prepared by treatment of m-ethylaniline (I) with cyanogen bromide (II) in Et2O.Alkylation of (III) with iodomethane and NaH provided the N-methyl cyanamide (IV).This was finally condensed with 1-naphthylamine hydrochloride (V) by heating at 160 C or in the presence of AlCl3 as the catalyst.
参考文献标题:Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives.N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: A new,selective noncompetitive NMDA receptor antagonist
文献作者:Reddy,N.L.; Hu,L.Y.; Cotter,R.E.; Fischer,J.B.; Wong,W.J.; McBurney,R.N.; Weber,E.; Holmes,D.L.; Wong,S.T.; Prasad,R.N.; et al.
参考来源:J Med Chem 1994,37(2),260
产品链接: CAS No. 137159-92-3›› 产品链接: CAS No.137160-11-3››