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“一锅”三组分合成新型1,5-苯并二氮杂䓬类化合物与抗牛病毒性腹泻病毒(BVDV)活性

韩超a, 聂磊a, 韩晓b, 张岩a, 孙克磊a, 石磊a, 崔光华a, 孟伟a   

  1. a 华北理工大学化学工程学院 唐山 063210;
    b 邯郸学院化学化工与材料学院 邯郸 056005
  • 收稿日期:2020-04-12 修回日期:2020-06-17 发布日期:2020-09-30
  • 通讯作者: 韩超 E-mail:hanchao@ncst.edu.cn
  • 基金资助:
    河北省自然科学基金委，青年基金项目（No.B2017209119）、河北省教育厅，河北省高等学校科学技术研究项目（No.Z2017013）资助项目.

Three-component one-pot synthesis of novel 1,5-benzodiazepine derivatives and their anti-BVDV activity

Chao Hana, Lei Niea, Xiao Hanb, Yan Zhanga, Kelei Suna, Lei Shia, Guanghua Cuia, Wei Menga   

  1. a College of Chemical Engineering, North China University of Science and Technology, Tangshan, 063210, China;
    b College of Chemical Engineering&Material, Handan University, Handan, 056005, China
  • Received:2020-04-12 Revised:2020-06-17 Published:2020-09-30
  • Supported by:
    Project supported by the Natural Science Foundation of Hebei Province of China (No. B2017209119) and the education department of Hebei Province of China (No. Z2017013).

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Supporting Info.

1

The "one-pot" three-component reaction is established to synthesize 1,5-benzodiazepine derivatives containing pyrrolidinone. These reactions were carried out readily with p-toluenesulfonic acid (p-TSA) as the catalyst in good yields. Reaction conditions were mild, environmental friendly. The benzodiazepine derivatives displayed prominent anti-BVDV activity with excellent EC50 values and no significant cytotoxicity. Our research could afford significative compounds for the research of anti-BVDV agents.

Key words: “one-pot” three-component reaction, 1,5-benzodiazepine derivatives, p-TSA, pyrrolidinone, anti-BVDV