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稻壳灰负载氯磺酸催化吡喃并[2,3-d]嘧啶的合成及抗菌活性研究

Rice husk ash supported chlorosulfonic acid as catalyst for synthesis and antibacterial activity of of pyrano [2,3-d] pyrimidines

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【作者】 雷英杰; 丁玫; 吴新世;

【Author】 LEI Ying-jie;DING Mei;WU Xin-shi;School of Chemistry&Chemical Engineering, Tianjin University of Technology,Tianjin key Laboratory of Drug Targeting and Bioimaging;

【通讯作者】 雷英杰;

【机构】 天津理工大学化学化工学院天津市药物靶向与生物成像重点实验室;

【摘要】 微波辅助下,以稻壳灰负载氯磺酸为固体酸催化剂,以芳香醛、丙二腈和二甲基环己二酮为原料进行"一锅法"缩合反应,所得到的中间体2-氨基-3-氰基苯并吡喃不需分离和纯化,直接加入乙酸酐继续缩合成环制备得到吡喃并[2,3-d]嘧啶衍生物(2a~2g),合成收率为83~92%,其结构经IR、~1HNMR、MS(EI)和元素分析等测试技术加以确证。初步的活性测试结果表明,部分目标化合物对大肠杆菌、枯草杆菌和金黄色葡萄球菌都有不同程度的抑制作用。

【Abstract】 A series of pyrano[2,3-d]pyrimidine derivatives(2 a~2 g)via the condensation reaction between acetic anhydride and 2-amino-3-cyano-4H-pyran derivatives were reported.The one-pot three-component condensation procedure was carried out by arylaldehydes with malononitrile and 5,5-dimethylcyclohexane-1,3-dione under microwave irradiation in the presence of rice husk ash supported chlorosulfonic acid and without purification, and with 83~92% yield respectively.The structures of the corresponding products were confirmed by IR,~1HNMR,MS(EI)and elemental analysis.Preliminary bioassay results showed that some of them had certain antibacterial activities against Escherichia Coli, Bacillus Subtilis and Staphylococcus Aureus.

  • 【文献出处】 化学研究与应用 ,Chemical Research and Application , 编辑部邮箱 ,2021年06期
  • 【分类号】O626
  • 【下载频次】74
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