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【结 构 式】 
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【分子编号】57816 【品名】N-[3-(4-chlorophenyl)-3-(2-pyridinyl)propyl]-4-[(1-trityl-1H-imidazol-4-yl)methyl]benzenecarboximidamide 【CA登记号】 |
【 分 子 式 】C44H38ClN5 【 分 子 量 】672.27212 【元素组成】C 78.61% H 5.7% Cl 5.27% N 10.42% |
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：(X)Metalation of 1-trityl-4-iodoimidazole (VI) with ethylmagnesium bromide, followed by addition to 4-cyanobenzaldehyde (VII) gives rise to the carbinol (VIII), which is further reduced to the diaryl methane (IX) employing triibutyltin hydride in the presence of AIBN. Trimethylaluminium-catalyzed coupling between nitrile (IX) and amine (V) provides amidine (X). The N-trityl group of (X) is finally removed under acidic conditions to furnish the title compound.
| 【1】 Tom, W.; Aslanian, R.; West, R.; Shih, N.-Y.; Piwinski, J.J.; She, S.; Williams, S.M.; Design and synthesis of novel dual histamine H1/H3 receptor antagonists based on the H1 receptor antagonist chlorpheniramine. 223rd ACS Natl Meet (April 7 2002, Orlando) 2002, Abst MEDI 63. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (V) | 57813 | 3-(4-chlorophenyl)-3-(2-pyridinyl)propylamine; 3-(4-chlorophenyl)-3-(2-pyridinyl)-1-propanamine | C14H15ClN2 | 详情 | 详情 | |
| (VI) | 30216 | 4-iodo-1-trityl-1H-imidazole | C22H17IN2 | 详情 | 详情 | |
| (VII) | 17552 | 4-formylbenzonitrile; 4-Cyanobenzaldehyde | 105-07-7 | C8H5NO | 详情 | 详情 |
| (VIII) | 57814 | 4-[hydroxy(1-trityl-1H-imidazol-4-yl)methyl]benzonitrile | C30H23N3O | 详情 | 详情 | |
| (IX) | 57815 | 4-[(1-trityl-1H-imidazol-4-yl)methyl]benzonitrile | C30H23N3 | 详情 | 详情 | |
| (X) | 57816 | N-[3-(4-chlorophenyl)-3-(2-pyridinyl)propyl]-4-[(1-trityl-1H-imidazol-4-yl)methyl]benzenecarboximidamide | C44H38ClN5 | 详情 | 详情 |
Extended Information