[1]马晓明,杨桂翔,杨泽熙,等.Huisgen [3+2]环加成/N-芳基化串联反应合成三氮唑苯二氮卓化合物[J].常州大学学报(自然科学版),2020,32(06):31-36,75.[doi:10.3969/j.issn.2095-0411.2020.06.005]
 MA Xiaoming,YANG Guixiang,YANG Zexi,et al.Synthesis of Triazolobenzodiazepine Analogs via Sequential Huisgen [3+2] Cycloaddition/N-Arylation Reactions[J].Journal of Changzhou University(Natural Science Edition),2020,32(06):31-36,75.[doi:10.3969/j.issn.2095-0411.2020.06.005]
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Huisgen [3+2]环加成/N-芳基化串联反应合成三氮唑苯二氮卓化合物()
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常州大学学报(自然科学版)[ISSN:2095-0411/CN:32-1822/N]

卷:
第32卷
期数:
2020年06期
页码:
31-36,75
栏目:
化学化工
出版日期:
2020-11-28

文章信息/Info

Title:
Synthesis of Triazolobenzodiazepine Analogs via Sequential Huisgen [3+2] Cycloaddition/N-Arylation Reactions
文章编号:
2095-0411(2020)06-0031-06
作者:
马晓明杨桂翔杨泽熙严生虎张跃
常州大学 药学院,江苏 常州 213164
Author(s):
MA Xiaoming YANG Guixiang YANG Zexi YAN Shenghu ZHANG Yue
School of Pharmacy, Changzhou University, Changzhou 213164, China
关键词:
Huisgen [3+2]环加成 N-芳基化反应 三氮唑苯二氮卓
Keywords:
Huisgen [3+2] cycloaddition N-arylation triazolobenzodiazepine
分类号:
O 626.4
DOI:
10.3969/j.issn.2095-0411.2020.06.005
文献标志码:
A
摘要:
研究了四氢吡咯并[3,4-c]吡咯-1,3-二酮经N-炔丙基化反应,铜催化的Huisgen [3+2]环加成和N-芳基化串联反应一步法合成三氮唑苯二氮卓化合物的新方法。产物经熔点仪、质谱、1H NMR和13C NMR进行了表征。该方法原料易得、操作简单、反应条件温和、产物收率高。
Abstract:
A novel and efficient approach is studied for the synthesis of triazolobenzodiazepine analogs by employing tetrahydropyrrolo[3,4-c]pyrrole-1,3-dione as the substrates, via sequential N-propargylation, Cu-catalyzed Huisgen [3+2] cycloadditon and N-arylation reactions. The desired products have been characterized by melting point, mass spectra, 1H NMR and 13C NMR. This procedure is conducted under mild reaction condition with simple substrates and easy operation to give corresponding products in high yield.

参考文献/References:


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备注/Memo

备注/Memo:
收稿日期:2020-07-28。
基金项目:江苏省产学研前瞻性联合研究资助项目(BY2015027-04)。
作者简介:马晓明(1984—),男,江苏无锡人,博士,讲师。E-mail:mxm.wuxi@cczu.edu.cn
更新日期/Last Update: 1900-01-01