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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 50, 2020 - Issue 23
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Articles

PPh3/I2-catalyzed one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones

Yanzhi Zhanga College of Pharmacy, Dali University, Dali, P.R. ChinaView further author information
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Min Leid Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaView further author information
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Kangsheng Xueb College of Pharmacy, Changchun University of Chinese Medicine, Changchun, P.R. ChinaView further author information
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Guoxiang Sunb College of Pharmacy, Changchun University of Chinese Medicine, Changchun, P.R. China;c School of Chemistry and Chemical Engineering, Yancheng Institute of Technology, Yancheng, P.R. ChinaView further author information
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Yang Zhoud Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaView further author information
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Jinjun Houd Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaView further author information
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Huali Longd Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaView further author information
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Zijia Zhangd Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaView further author information
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Xubing Chena College of Pharmacy, Dali University, Dali, P.R. ChinaCorrespondence[email protected]
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Wanying Wud Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China;e University of Chinese Academy of Sciences, Beijing, P.R. ChinaCorrespondence[email protected]
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Pages 3661-3668 | Received 09 Feb 2020, Published online: 08 Sep 2020
 
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Abstract

A method using PPh3/I2-catalyzed three-component Biginelli reaction of aromatic ketone, aromatic aldehyde and urea to synthesize4,6-diarylpyrimidin-2-(1H)-ones is described. Under the experimental conditions, the main reaction products are 4,6-diarylpyrimidin-2-(1H)-ones not 4,6-diaryl-3,4-dihydropyrimidin-2(1H)-ones. The advantage of this method is to achieve improved product yields with an inexpensive and readily available catalyst, and easy experimental set-up, which provides a good method to synthesize 4,6-diarylpyrimidin-2-(1H)-ones.

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Additional information

Funding

This work was supported by Special Fund for Strategic Pilot Technology Chinese Academy of Sciences [XDA12020379], the National Natural Science Foundation of China [grants 81973455], National Key R&D Program of China [2018YFC1707900].

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