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项目整合精选>>>Emedastine difumarate, Emedastine fumarate, AL-3432A, KG-2413, LY-188695, KB-2413, Emadine(as ophthalmic formulation), Rapimine, Remicut, Daren
Emedastine difumarate, Emedastine fumarate, AL-3432A, KG-2413, LY-188695, KB-2413, Emadine(as ophthalmic formulation), Rapimine, Remicut, Daren
富马酸依美斯汀依美司丁Chemical Name: 1-(2-Ethoxyethyl)-2-(4-methyl-hexahydro-1H-1,4-diazepin-1-yl)-1H-benzimidazole (E)-2-butenedioate (1:2); 1-(2-Ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate
CAS No. 87233-62-3, 87233-76-9 ((2:3) salt), 87233-61-2 (free base)
项目整合开发状态: Launched-1993
项目研究机构: Kanebo (Originator), Alcon (Licensee), Kowa (Licensee)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Benzimidazole derivatives,process for the peparation thereof and pharmaceutical composition containing the same
文献作者:Iemura,R.; et al.(Kanebo Pharmaceuticals,Ltd.)
参考来源:EP 0079545; JP 58079983
📄 详细内容
合成路线: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.
参考文献标题:KB-2413
文献作者:Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1985,10(5),397
合成路线: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.
参考文献标题:Synthesis of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)-[2-14C]benzimidazole difumarate ([14C]KB-2413)
文献作者:Awata,N.; Satomi,O.
参考来源:J Label Compd Radiopharm 1987,24(3),331-8
产品链接: CAS No. 87233-62-3›› 产品链接: CAS No.87233-61-2››