期刊
CHEMICAL SCIENCE
卷 -, 期 -, 页码 -出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1sc01891d
关键词
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资金
- Singapore National Research Foundation [NRF-NRFI2016-06, NRF-CRP22-2019-0002]
- Ministry of Education, Singapore [RG108/16, RG5/19, RG1/18, MOE2019-T2-2-117, MOE2018-T3-1-003]
- Agency for Science, Technology and Research (A* STAR) under its A*STAR AME IRG Award [A1783c0008, A1783c0010]
- GSK-EDB Trust Fund
- Nanyang Technological University
- National Natural Science Foundation of China [21772029, 21801051, 21807019, 21961006, 22071036, 22061007, 82360589, 81360589, 31960546]
- Frontiers Science Center for Asymmetric Synthesis and Medicinal Molecules, Department of Education, Guizhou Province [(2020) 004]
- 10 Talent Plan (Shicengci) of Guizhou Province [[2016] 5649]
- Science and Technology Department of Guizhou Province [[2018]2802, [2019]1020]
- Program of Introducing Talents of Discipline to Universities of China (111 Program) at Guizhou University [D20023]
- Guizhou Province First-Class Disciplines Project (Yiliu Xueke Jianshe Xiangmu) [GNYL(2017)008]
- NSFC [81360589]
- Guizhou University of Traditional Chinese Medicine (China)
- Guizhou University
An efficient protocol has been developed for the synthesis of important aryl-dihydropyridazinone molecules, utilizing specific reaction steps to achieve the desired products. These molecules can be easily transformed into drugs and bioactive compounds.
4,5-Dihydropyridazinones bearing an aryl substituent at the C6-position are important motifs in drug molecules. Herein, we developed an efficient protocol to access aryl-dihydropyridazinone molecules via carbene-catalyzed asymmetric annulation between dinucleophilic arylidene hydrazones and bromoenals. Key steps in this reaction include polarity-inversion of aryl aldehyde-derived hydrazones followed by chemo-selective reaction with enal-derived alpha,beta-unsaturated acyl azolium intermediates. The aryl-dihydropyridazinone products accessed by our protocol can be readily transformed into drugs and bioactive molecules.
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