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【结 构 式】 
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【药物名称】 【化学名称】N-[4-(2-Benzothiazolyl)phenyl]-N-[11C]methylamine 【CA登记号】 【 分 子 式 】C14H12N2S 【 分 子 量 】239.31799 |
【开发单位】University of Pittsburgh (Originator) 【药理作用】Diagnostic Agents, Diagnostic for Alzheimer's Disease, Radiopharmaceuticals, Radiopharmaceuticals for Brain Imaging |
合成路线1
Condensation of 2-aminothiophenol (I) with 4-nitrobenzoyl chloride (II) produces the benzothiazole (III). Reduction of the nitro group of (III) by means of SnCl2 in refluxing EtOH yields aniline (IV). Then, alkylation of (IV) with 11C-labeled iodomethane gives rise to the target 11C-methylated aniline.
| 【1】 Mathis, C.A.; et al.; A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain. Bioorg Med Chem Lett 2002, 12, 3, 295. |
| 【2】 Wang, Y.; Klunk, W.E.; Mathis, C.A. Jr. (University of Pittsburgh); Thioflavin derivs. for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition. WO 0216333 . |
| 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) | 25182 | 2-aminobenzenethiol | 137-07-5 | C6H7NS | 详情 | 详情 |
| (II) | 18941 | p-nitrobenzoyl chloride; 4-nitrobenzoyl chloride | 122-04-3 | C7H4ClNO3 | 详情 | 详情 |
| (III) | 58508 | 2-(4-nitrophenyl)-1,3-benzothiazole | C13H8N2O2S | 详情 | 详情 | |
| (IV) | 58509 | 4-(1,3-benzothiazol-2-yl)aniline; 4-(1,3-benzothiazol-2-yl)phenylamine | C13H10N2S | 详情 | 详情 |
Extended Information