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【结 构 式】

【分子编号】57814

【品名】4-[hydroxy(1-trityl-1H-imidazol-4-yl)methyl]benzonitrile

【CA登记号】

【 分 子 式 】C30H23N3O

【 分 子 量 】441.53224

【元素组成】C 81.61% H 5.25% N 9.52% O 3.62%

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:(VIII)

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