【药物名称】Emedastine difumarate, Emedastine fumarate, AL-3432A, KG-2413, LY-188695, KB-2413, Emadine(as ophthalmic formulation), Rapimine, Remicut, Daren
化学结构式(Chemical Structure):
参考文献No.46342
标题:Benzimidazole derivatives, process for the peparation thereof and pharmaceutical composition containing the same
作者:Iemura, R.; et al. (Kanebo Pharmaceuticals, Ltd.)
来源:EP 0079545; JP 58079983
合成路线图解说明:

The reaction of 2-chlorobenzimidazole (I) with 2-chloroethyl ethyl ether (II) by means of NaOH in DMF gives 1-(2-ethoxyethyl)benzimidazole (III), which is then condensed with N-methylhomopiperazine (IV) at 120 C.

参考文献No.65722
标题:KB-2413
作者:Serradell, M.N.; Casta馿r, J.
来源:Drugs Fut 1985,10(5),397
合成路线图解说明:

The reaction of 2-chlorobenzimidazole (I) with 2-chloroethyl ethyl ether (II) by means of NaOH in DMF gives 1-(2-ethoxyethyl)benzimidazole (III), which is then condensed with N-methylhomopiperazine (IV) at 120 C.

参考文献No.76442
标题:Synthesis of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)-[2-14C]benzimidazole difumarate ([14C]KB-2413)
作者:Awata, N.; Satomi, O.
来源:J Label Compd Radiopharm 1987,24(3),331-8
合成路线图解说明:

A new synthesis of KB-2413 has been described: The reaction of 2-chloronitrobenzene (I) with 2-ethoxyethylamine (II) gives 1-(2-ethoxyethylamino)-2-nitrobenzene (III), which is reduced with Zn and NaOH to N-(2-ethoxyethyl-o-phenylenediamine (IV). The cyclization of (IV) with urea in amyl alcohol affords 1-(2-ethoxyethyl)benzimidazol-2-one (V), which is treated with refluxing POCl3 yielding 2-chloro-1-(2-ethoxyethyl)benzimidazole (VI). Finally, this compound is condensed with N-methylhexahydro-1,4-diazepine (VII) and treated with fumaric acid.

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