Journal
CHINESE JOURNAL OF ORGANIC CHEMISTRY
Volume 41, Issue 2, Pages 819-825Publisher
SCIENCE PRESS
DOI: 10.6023/202004018
Keywords
one-pot three-component reaction; 1,5-benzodiazepine derivatives; p-TSA; pyrrolidinone; anti-BVDV
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Funding
- Natural Science Foundation of Hebei Province [B2017209119]
- Education Department of Hebei Province [Z2017013]
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A one-pot three-component reaction was developed to synthesize 1,5-benzodiazepine derivatives with pyrrolidinone, showing significant anti-BVDV activity with good safety profiles. This method provides a promising strategy for the research of anti-BVDV agents.
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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