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【结 构 式】 
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【分子编号】61781 【品名】2-chloro-3-(4-fluorobenzyl)-1-[(2-methoxyethoxy)methyl]-3H-benzimidazol-1-ium bromide 【CA登记号】 |
【 分 子 式 】C18H19BrClFN2O2 【 分 子 量 】429.7162432 【元素组成】C 50.31% H 4.46% Br 18.59% Cl 8.25% F 4.42% N 6.52% O 7.45% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(III)The condensation of 2-chloro-1-(4-fluorobenzyl)-1H-benzimidazole (I) with 2-methoxyethoxymethyl bromide (II) in toluene gives the benzimidazolium bromide (III), which is condensed with 1-acetyl-4-aminopiperidine (IV) in hot toluene to yield the adduct (V). Finally, this compound is treated first with BBr3 in dichloromethane and then with HBr or HCl at 110 C to provide the target Norastemizole.
| 【1】 Hong, Y.; Senanayake, C.H.; Bakale, R.P. (Sepracor Inc.); Methods for synthesizing 2-substd. imidazoles. EP 0977740; JP 2001520658; US 5817823; WO 9846571 . |
| 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) | 12043 | 1-(4-Fluorobenzyl-2-chlorobenzimidazol; 2-Chloro-1-(4-fluorobenzyl)-1H-benzimidazole; 1-(4-Fluorobenzyl)-2-chlorobenzimidazole | 84946-20-3 | C14H10ClFN2 | 详情 | 详情 |
| (II) | 61780 | 1-(bromomethoxy)-2-methoxyethane; 2-(bromomethoxy)ethyl methyl ether | C4H9BrO2 | 详情 | 详情 | |
| (III) | 61781 | 2-chloro-3-(4-fluorobenzyl)-1-[(2-methoxyethoxy)methyl]-3H-benzimidazol-1-ium bromide | C18H19BrClFN2O2 | 详情 | 详情 | |
| (IV) | 61782 | 1-(4-amino-1-piperidinyl)-1-ethanone | C7H14N2O | 详情 | 详情 | |
| (V) | 61783 | 2-[(1-acetyl-4-piperidinyl)amino]-3-(4-fluorobenzyl)-1-[(2-methoxyethoxy)methyl]-3H-benzimidazol-1-ium bromide | C25H32BrFN4O3 | 详情 | 详情 |
Extended Information