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【结 构 式】 
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【分子编号】61777 【品名】2-chloro-3-(4-fluorobenzyl)-1-(methoxymethyl)-3H-benzimidazol-1-ium 【CA登记号】 |
【 分 子 式 】C16H15ClFN2O 【 分 子 量 】305.7590832 【元素组成】C 62.85% H 4.94% Cl 11.59% F 6.21% N 9.16% O 5.23% |
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 methoxymethyl bromide (II) in toluene gives the benzimidazolium bromide (III), which is condensed with 4-aminopiperidine-1-carboxylic acid ethyl ester (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) | 19619 | bromo(methoxy)methane; bromomethyl methyl ether | 13057-17-5 | C2H5BrO | 详情 | 详情 |
| (III) | 61777 | 2-chloro-3-(4-fluorobenzyl)-1-(methoxymethyl)-3H-benzimidazol-1-ium | C16H15ClFN2O | 详情 | 详情 | |
| (IV) | 61778 | propyl 4-amino-1-piperidinecarboxylate | C9H18N2O2 | 详情 | 详情 | |
| (V) | 61779 | 3-(4-fluorobenzyl)-1-(methoxymethyl)-2-{[1-(propoxycarbonyl)-4-piperidinyl]amino}-3H-benzimidazol-1-ium bromide | C25H32BrFN4O3 | 详情 | 详情 |
Extended Information