Chin. J. Org. Chem. ›› 2007, Vol. 27 ›› Issue (11): 1369-1373. Previous Articles     Next Articles

Original Articles



  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

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