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【结 构 式】 
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【药物名称】Pittsburgh Compound B, PIB, 6-OH-BTA-1 【化学名称】2-[4-(Methylamino)phenyl]benzothiazol-6-ol 【CA登记号】566170-04-5 【 分 子 式 】C14H12N2OS 【 分 子 量 】256.32854 |
【开发单位】University of Pittsburgh (Originator), Uppsala University (Codevelopment) 【药理作用】Diagnostic Agents, Diagnostic for Alzheimer's Disease |
合成路线1
Condensation of 2-amino-5-methoxythiophenol (I) with 4-(methylamino)benzoic acid (II) in hot polyphosphoric acid produces the benzothiazole derivative (III), which is finally submitted to methyl ether cleavage by means of BBr3 to give the target hydroxy compound.
| 【1】 Mathis, C.A.; Wang, Y.; Holt, D.P.; Huang, G.-F.; Debnath, M.L.; Klunk, W.E.; Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem 2003, 46, 13, 2740. |
| 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) | 25876 | 2-amino-5-methoxyphenylhydrosulfide; 5-Methoxy-2-aminothiophenol;2-Mercapto-4-methoxyaniline;2-amino-5-methoxybenzenethiol；2-Amino-5-methoxy-1-benzenethiol | 6274-29-9 | C7H9NOS | 详情 | 详情 |
| (II) | 64844 | 4-(methylamino)benzoic acid | C8H9NO2 | 详情 | 详情 | |
| (III) | 64845 | 4-(6-methoxy-1,3-benzothiazol-2-yl)-N-methylaniline; N-[4-(6-methoxy-1,3-benzothiazol-2-yl)phenyl]-N-methylamine | C15H14N2OS | 详情 | 详情 |
Extended Information