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4,5-二芳基-3,4-二氢嘧啶-2(1)-酮的高效合成:碳酸铯促进的1-芳基-2-丙酮与1,1'-(芳基亚甲基)二脲的直接缩合反应。

An efficient synthesis of 4,5-diaryl-3,4-dihydropyrimidin-2(1)-one a cesium carbonate-promoted direct condensation of 1-aryl-2-propanone with 1,1'-(arylmethylene)diurea.

作者信息

Guo Yi-Cong, Song Xuan-Di, Deng Wei, Rao Weidong, Xu Haiyan, Shen Zhi-Liang

机构信息

Institute of Advanced Synthesis, School of Chemistry and Molecular Engineering, Nanjing Tech University Jiangsu 211816 China

Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-Forest Biomass, College of Chemical Engineering, Nanjing Forestry University Nanjing 210037 China.

出版信息

RSC Adv. 2020 Aug 14;10(50):30062-30068. doi: 10.1039/d0ra05480a. eCollection 2020 Aug 10.

Abstract

An efficient method for the synthesis of 4,5-diaryl-3,4-dihydropyrimidin-2(1)-one by using 1,1'-(arylmethylene)diurea and 1-aryl-2-propanone as substrates was developed. The reactions proceeded efficiently in the presence of CsCO to give the desired products in moderate to good yields with wide substrate scope and good functional group tolerance, serving as an attractive alternative or complement to the previously reported methods for the facile assembly of biologically and pharmaceutically active 3,4-dihydropyrimidin-2(1)-ones.

摘要

开发了一种以1,1'-(芳基亚甲基)二脲和1-芳基-2-丙酮为底物合成4,5-二芳基-3,4-二氢嘧啶-2(1)-酮的有效方法。该反应在碳酸铯存在下高效进行,能以中等至良好的产率得到所需产物,底物范围广,官能团耐受性好,是先前报道的用于简便组装具有生物和药物活性的3,4-二氢嘧啶-2(1)-酮方法的有吸引力的替代或补充方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a35a/9056278/d57aba8c3c92/d0ra05480a-s1.jpg

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