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【结 构 式】 
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【药物名称】IMPY 【化学名称】N-[4-[6-([125I]-Iodo)imidazo[1,2-a]pyridin-2-yl]phenyl]-N,N-dimethylamine 【CA登记号】474012-78-7, 474012-75-4 (unlabeled) 【 分 子 式 】C15H14IN3 【 分 子 量 】361.29893 |
【开发单位】University of Pennsylvania (Originator), University of Toronto (Originator), Washington University (Originator) 【药理作用】Diagnostic Agents, Diagnostic for Alzheimer's Disease, Antiamyloidogenic Agents |
合成路线1
Condensation between 2-bromo-4'-(dimethylamino)acetophenone (I) and 2-amino-5-bromopyridine (II) gives rise to the imidazopyridine (III). Subsequent palladium-catalyzed stannylation of (III) affords the tributyltin derivative (IV). The target radio-iodinated compound is then obtained by iododstannylation of (IV) with [125I] iodide in the presence of H2O2 (1,2)
| 【1】 Zhuang, Z.-P.; Kung, M.-P.; Wilson, A.; Lee, C.-W.; Plossl, K.; Hou, C.; Holtzman, D.M.; Kung, H.F.; Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain. J Med Chem 2003, 46, 2, 237. |
| 【2】 Kung, H.; Kung, M.-P.; Zhuang, Z.-P. (University of Pennsylvania); Amyloid plaque aggregation inhibitors and diagnostic imaging agents. CA 2444214; EP 1381604; US 2003059369; WO 0285903 . |
| 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) | 63545 | 2-bromo-1-[4-(dimethylamino)phenyl]-1-ethanone | C10H12BrNO | 详情 | 详情 | |
| (II) | 12123 | 5-Bromo-2-pyridinylamine; 5-Bromo-2-pyridinamine; 2-Amino-5-bromopyridine | 1072-97-5 | C5H5BrN2 | 详情 | 详情 |
| (III) | 63546 | 4-(6-bromoimidazo[1,2-a]pyridin-2-yl)-N,N-dimethylaniline; N-[4-(6-bromoimidazo[1,2-a]pyridin-2-yl)phenyl]-N,N-dimethylamine | C15H14BrN3 | 详情 | 详情 | |
| (IV) | 63547 | N,N-dimethyl-4-[6-(tributylstannyl)imidazo[1,2-a]pyridin-2-yl]aniline; N,N-dimethyl-N-{4-[6-(tributylstannyl)imidazo[1,2-a]pyridin-2-yl]phenyl}amine | C27H41N3Sn | 详情 | 详情 |
Extended Information