Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (6): 1370-1374.DOI: 10.6023/cjoc201412053 Previous Articles     Next Articles



冯俊娜a,b, 李晓慧c, 邵洁a, 朱墨a, 李妍a, 陈华a, 李小六a   

  1. a 河北大学化学与环境科学学院 河北省化学生物学重点实验室 保定 071002;
    b 中国地质大学长城学院 地球科学与资源系 保定 071000;
    c 河北农业大学理学院 保定 071001
  • 收稿日期:2014-12-30 修回日期:2015-02-03 发布日期:2015-02-05
  • 通讯作者: 陈华, 李小六;
  • 基金资助:

    国家自然科学基金(No. 21372060)、河北省自然科学基金石药集团医药联合基金(No. B2012201113)、河北省教育厅自然科学基金(No. Y2011119)、保定市科技局(No. 14ZF095)资助项目.

Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones

Feng Junnaa,b, Li Xiaohuic, Shao Jiea, Zhu Moa, Li Yana, Chen Huaa, Li Xiaoliua   

  1. a Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002;
    b Department of the Earth Sciences and Resources, China University of Geosciences Great Wall College, Baoding 071000;
    c College of Sciences, Agricultural University of Hebei, Baoding 071001
  • Received:2014-12-30 Revised:2015-02-03 Published:2015-02-05
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21372060), the Medicinal Joint Funds of the Natural Science Foundation of Hebei and Shijiazhuang Pharmaceutical Group (No. B2012201113), the Natural Science Foundations of Education Department of Hebei (No. Y2011119), and the Foundations of Baoding City Science and Technology Bureau (No. 14ZF095).

A series of novel diaryl benzothiazin-4-ones were designed and synthesized by the three-component one-pot cyclocondensation of pyrimidinamine, aromatic aldehyde and thiosalicylic acid under microwave irradiation for 10 min. The reaction has the advantages such as short reaction time and simple operation. The structures of the newly synthesized compounds were confirmed by IR, NMR, MS spectra and elemental analysis. The compound 2-(2,6-dichlorophenyl)-3-(4,6-di- methylpyrimidin-2-yl)-2H-benzo[e][1,3]thiazin-4(3H)-one (10c) could effectively inhibit HIV-RT activity with the IC50 value of 8.38 祄ol·L-1, the others showed middle RT inhibitory activity.

Key words: benzothiazin-4-one, anti-HIV-RT activity, microwave irradiation