【药物名称】Aptiganel, CNS-1102, Cerestat(former Brand Name)
化学结构式(Chemical Structure):
参考文献No.23334
标题:Tri- and tetra-substd. guanidines and their use as excitatory amino acid antagonists
作者:Weber, E.; Keana, J.F.W. (University of Oregon)
来源:JP 2002020361; US 5262568; WO 9112797
合成路线图解说明:

(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No.34149
标题:Preparation of substd. guanidines
作者:Durant, G.J.; Nagar, S.S. (CeNeS Pharmaceuticals)
来源:WO 9319042
合成路线图解说明:

(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No.241894
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
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.
来源:J Med Chem 1994,37(2),260
合成路线图解说明:

(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.

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