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【结 构 式】 
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【药物名称】TZDM 【化学名称】N-[4-(6-[125I]Iodobenzothiazol-2-yl)phenyl]-N,N-dimethylamine 【CA登记号】 【 分 子 式 】C15H13IN2S 【 分 子 量 】378.34826 |
【开发单位】University of Pennsylvania (Originator) 【药理作用】Diagnostic Agents, Diagnostic for Alzheimer's Disease |
合成路线1
The cyclization of 4-bromo-2-sulfanylaniline (I) with 4-(dimethylamino)benzaldehyde (II) by heating at 180 C in DMSO gives 6-bromo-2-[4-(dimethylamino)phenyl]benzothiazole (III), which is treated with (Bu3Sn)2 (IV) and Pd(PPh3)4 and TEA in dioxane to yield the tributyltin derivative (V). Finally, this compound is treated with 125INa and H2O2 in ethanol/water to afford the target radiolabeled compound.
| 【1】 Zhuang, Z.-P.; et al.; Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates. J Med Chem 2001, 44, 12, 1905. |
| 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) | 25571 | 2-amino-5-bromobenzenethiol; 2-amino-5-bromophenylhydrosulfide | C6H6BrNS | 详情 | 详情 | |
| (II) | 17771 | N,N-Dimethyl-p-aminobenzaldehyde; Ehrlich's reagent; p-Dimethylaminobenzaldehyde; 4-(dimethylamino)benzaldehyde | 100-10-7 | C9H11NO | 详情 | 详情 |
| (III) | 52427 | N-[4-(6-bromo-1,3-benzothiazol-2-yl)phenyl]-N,N-dimethylamine; 4-(6-bromo-1,3-benzothiazol-2-yl)-N,N-dimethylaniline | C15H13BrN2S | 详情 | 详情 | |
| (IV) | 52428 | Bis(tributyltin); Hexabutyldistannane; Bis(tri-n-butyltin); Hexa-n-butylditin; Hexa-n-butyldistannane | 813-19-4 | C24H54Sn2 | 详情 | 详情 |
| (V) | 52429 | N,N-dimethyl-N-{4-[6-(tributylstannanyl)-1,3-benzothiazol-2-yl]phenyl}amine; N,N-dimethyl-4-[6-(tributylstannanyl)-1,3-benzothiazol-2-yl]aniline | C27H40N2SSn | 详情 | 详情 |
Extended Information