BOM-1006
Chemical Name: 2,3,6-Trimethyl-4-[2-[2-[2-(4-methyl-1,4-perhydrodiazepin-1-yl)-1H-benzimidazol-1-yl]ethoxy]ethoxy]phenol difumarate
CAS No. 256366-95-7, 256366-84-4 (free base)
项目整合开发状态: Preclinical
项目研究机构: Fuji Yakuhin (Originator)
合成路线:2-Chlorobenzimidazole (I) was treated with NaH in DMF and the resulting sodium salt was alkylated with 4-[2-(2-chloroethoxy)ethoxy]-2,3,6-trimethylphenol (II) to give (III).Subsequent displacement of the chlorine of (III) with N-methyl homopiperazine (IV) at 130 C produced the desired 2-(homopiperazino)benzimidazole,which was finally treated with fumaric acid in EtOH to yield the corresponding bis fumarate salt.
📌 参考资料/链接：
参考文献标题:Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action
文献作者:Nakano,H.; Inoue,T.; Kawasaki,N.; Miyataka,H.; Matsumoto,H.; Taguchi,T.; Inagaki,N.; Nagai,H.; Satoh,T.
参考来源:Chem Pharm Bull 1999,47(11),1573
📄 详细内容
合成路线:2-Chlorobenzimidazole (I) was treated with NaH in DMF and the resulting sodium salt was alkylated with 4-[2-(2-chloroethoxy)ethoxy]-2,3,6-trimethylphenol (II) to give (III).Subsequent displacement of the chlorine of (III) with N-methyl homopiperazine (IV) at 130 C produced the desired 2-(homopiperazino)benzimidazole,which was finally treated with fumaric acid in EtOH to yield the corresponding bis fumarate salt.
参考文献标题:Synthesis and biological activities of novel antiallergic agents with 5-lipoxygenase inhibiting action
文献作者:Nakano,H.; Inoue,T.; Kawasaki,N.; Miyataka,H.; Matsumoto,H.; Taguchi,T.; Inagaki,N.; Nagai,H.; Satoh,T.
参考来源:Bioorg Med Chem 2000,8(2),373