|
【结 构 式】 
|
【药物名称】BOM-1006 【化学名称】2,3,6-Trimethyl-4-[2-[2-[2-(4-methyl-1,4-perhydrodiazepin-1-yl)-1H-benzimidazol-1-yl]ethoxy]ethoxy]phenol difumarate 【CA登记号】256366-95-7, 256366-84-4 (free base) 【 分 子 式 】C34H44N4O11 【 分 子 量 】684.74998 |
【开发单位】Fuji Yakuhin (Originator) 【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, Atopic Dermatitis, Agents for, DERMATOLOGIC DRUGS, Drugs for Allergic Rhinitis, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Histamine H1 Antagonists, Lipoxygenase Inhibitors |
合成路线1
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.
| 【1】 Nakano, H.; Inoue, T.; Inagaki, N.; Taguchi, T.; Satoh, T.; Kawasaki, N.; Nagai, H.; Matsumoto, H.; Miyataka, H.; Synthesis and biological activities of novel antiallergic agents with 5-lipoxygenase inhibiting action. Bioorg Med Chem 2000, 8, 2, 373. |
| 【2】 Nakano, H.; Inoue, T.; Inagaki, N.; Taguchi, T.; Matsumoto, H.; Satoh, T.; Miyataka, H.; Kawasaki, N.; Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action. Chem Pharm Bull 1999, 47, 11, 1573. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 26761 | 2-chloroimidazo[1,2-a]pyridine; 2-chlorobenzimidazole; 2-Amino-4'-chlorodiphenylether; 2-Aminodiphenylether; 2-chloro-1H-benzimidazole | 4857-06-1 | C7H5ClN2 | 详情 | 详情 |
| (II) | 38944 | 4-[2-(2-chloroethoxy)ethoxy]-2,3,6-trimethylphenol | C13H19ClO3 | 详情 | 详情 | |
| (III) | 38945 | 4-[2-[2-(2-chloro-1H-benzimidazol-1-yl)ethoxy]ethoxy]-2,3,6-trimethylphenol | C20H23ClN2O3 | 详情 | 详情 | |
| (IV) | 20903 | 1-methyl-1,4-diazepane | 4318-37-0 | C6H14N2 | 详情 | 详情 |