有机化学 ›› 2021, Vol. 41 ›› Issue (2): 819-825.DOI: 10.6023/202004018 上一篇    下一篇

研究论文

“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, 崔广华a, 孟伟a,*()   

  1. a 华北理工大学化学工程学院 河北唐山 063210
    b 邯郸学院化学化工与材料学院 河北邯郸 056005
  • 收稿日期:2020-04-12 修回日期:2020-06-17 发布日期:2020-09-29
  • 通讯作者: 韩超, 孟伟
  • 作者简介:
    * Corresponding authors. E-mail: ;
  • 基金资助:
    河北省自然科学基金(B2017209119); 河北省教育厅基金(Z2017013)

One-Pot Three-Component Synthesis of Novel 1,5-Benzodiazepine Derivatives and Their anti-BVDV (Bovine Viral Diarrhea Virus) 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, Hebei 063210
    b College of Chemical Engineering & Material, Handan University, Handan, Hebei 056005
  • Received:2020-04-12 Revised:2020-06-17 Published:2020-09-29
  • Contact: Chao Han, Wei Meng
  • Supported by:
    the Natural Science Foundation of Hebei Province(B2017209119); the Education Department of Hebei Province(Z2017013)

以特氨酸、邻苯二胺和芳香醛为原料, 乙醇为溶剂, 对甲苯磺酸为催化剂, 多组分一锅法构建了一系列含有吡咯烷酮的1,5-苯并二氮杂?类化合物. 该方法反应条件温和, 操作简单, 产物收率高. 探索了抗牛病毒性腹泻病毒(BVDV)病毒活性, 结果显示合成的苯二氮?类衍生物具有显著的抗BVDV活性, EC50值好, 且无明显的细胞毒性, 为抗BVDV制剂的研究提供了有意义的参考物.

关键词: “一锅”三组分反应, 1, 5-苯并二氮杂?类化合物, 对甲苯磺酸, 吡咯烷酮, 抗BVDV

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, and environmental friendly. The benzodiazepine derivatives displayed prominent anti-BVDV (bovine viral diarrhea virus) 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