“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
收稿日期: 2020-04-12
修回日期: 2020-06-17
网络出版日期: 2020-09-29
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
Received date: 2020-04-12
Revised date: 2020-06-17
Online published: 2020-09-29
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
韩超 , 聂磊 , 韩晓 , 张岩 , 孙克磊 , 石磊 , 崔广华 , 孟伟 . “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[J]. 有机化学, 2021 , 41(2) : 819 -825 . DOI: 10.6023/202004018
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.
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