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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (11): 1369-1373. 上一篇    下一篇

研究论文

6-取代苯并噻唑苯胺类化合物的合成

郑明强a,b，尹端沚*,a，沈玉梅a，李谷才a   

  1. (a中国科学院上海应用物理研究所 放射性药物研究中心 上海 201800)
    (b中国科学院研究生院 北京 100049)
  • 收稿日期:2006-09-13 修回日期:2007-02-07 发布日期:2007-10-20
  • 通讯作者: 尹端沚

Syntheses of 2-(p-Aminophenyl)-6-substituent-benzothiazoles

ZHENG Ming-Qianga,b,YIN Duan-Zhi*,a,SHEN YU-Meia,LI Gu-Caia   

  1. (a Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics,
    Chinese Academy of Sciences, Shanghai 201800)
    (b Gradmate School of the Chinese Academy of Sciences, Beijing 100049)
  • Received:2006-09-13 Revised:2007-02-07 Published:2007-10-20
  • Contact: YIN Duan-Zhi

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被引次数

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以2-氨基苯并噻唑类化合物为原料, 通过碱性条件下水解, 与苯甲酸类化合物在PPA(聚磷酸)条件下脱水环化, 部分化合物通过BBr3去甲基化反应, 合成了一系列潜在的针对β-淀粉样蛋白的正电子放射性探针分子前体或作为参比的6-取代苯并噻唑苯胺类化合物, 并用1H NMR, IR, EI/ESI-MS, HRMS, 元素分析等对其进行了表征. 同时测定比较了6种化合物与早老性痴呆(Alzheimer’s disease, AD)死者脑匀浆的亲和力强弱.

关键词: 6-取代苯并噻唑苯胺类化合物, β-淀粉样蛋白, 合成, 亲和力, 表征

A series of novel 2-(p-aminophenyl)-6-substituent-benzothiazole derivatives as potential β-amyloid PET (positron emission tomography) tracers were prepared from proper 2-amino-6-substituted benzothiazoles through basic hydrolysis, intermolecular cycloaddition and N/O-alkylation reactions. Their structures were confirmed by IR, 1H NMR, EI/ESI-MS, HRMS spectra and elemental analysis. The sequence of binding affinities of some compounds with human brain homogenate was analyzed.

Key words: β-amyloid, synthesis, bind-ing affinity, characterization, 2-(p-aminophenyl)-6-substituent-benzothiazole