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【结 构 式】

【分子编号】21253

【品名】N-(tert-butyl)-4-[1-hydroxy-4-[1-(trimethylsilyl)-1H-imidazol-4-yl]butyl]benzamide

【CA登记号】

【 分 子 式 】C21H33N3O2Si

【 分 子 量 】387.59754

【元素组成】C 65.08% H 8.58% N 10.84% O 8.26% Si 7.25%

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:(IX)

2) The protection of 4-[3-(ethoxycarbonyl)propyl-1H-imidazole (VI) with trimethylsilyl chloride followed by reduction with diisobutylaluminum hydride (DBAH) in dichloromethane gives 4-(3-formylpropyl)-1-(trimethylsilyl)imidazole (VII), which is condensed with 4-(tert-butylcarbamoyl)bromobenzene (VIII) by means of butyllithium in THF yielding 4-[4-[4-(tert-butylcarbamoyl)phenyl]-4-hydroxybutyl]-1-(trimethylsilyl) imidazole (IX). The reaction of (IX) with refluxing SOCl2 affords 4-[4-chloro-4-(4-cyanophenyl)butyl]-1H-imidazole (X), which is finally cyclized in refluxing CHCl3.

1 Browne, L.J. (Ciba Geigy Corp.); Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors.. ES 8801262; JP 61012688; US 4617307 .
2 Pento, J.T.; Prous, J.; Castaner, J.; CGS-16949A. Drugs Fut 1989, 14, 9, 843.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VI) 21250 ethyl 4-(1H-imidazol-4-yl)butanoate C9H14N2O2 详情 详情
(VII) 21251 4-[1-(trimethylsilyl)-1H-imidazol-4-yl]butanal C10H18N2OSi 详情 详情
(VIII) 21252 4-bromo-N-(tert-butyl)benzamide C11H14BrNO 详情 详情
(IX) 21253 N-(tert-butyl)-4-[1-hydroxy-4-[1-(trimethylsilyl)-1H-imidazol-4-yl]butyl]benzamide C21H33N3O2Si 详情 详情
(X) 21254 4-[1-chloro-4-(1H-imidazol-4-yl)butyl]benzonitrile C14H14ClN3 详情 详情
Extended Information