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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (06): 876-883. 上一篇    下一篇

综述与进展

Biginelli 3,4-二氢嘧啶-2-酮衍生物的合成研究新进展

权正军 ; 张 彰 ; 达玉霞; 王喜存*   

  1. (西北师范大学化学化工学院 甘肃省高分子材料重点实验室 兰州 730070)
  • 收稿日期:2008-06-26 修回日期:2008-09-12 发布日期:2009-06-20
  • 通讯作者: 王喜存

New Advances in the Synthesis of Biginelli 3,4-Dihydropyrimidin-2(1H)-one Derivatives

Quan, Zhengjun ; Zhang, Zhang; Da, Yuxia; Wang, Xicun*   

  1. (Gansu Key Laboratory of Polymer Materials, College of Chemistry and Chemical Engineering,
    Northwest Normal University, Lanzhou 730070)
  • Received:2008-06-26 Revised:2008-09-12 Published:2009-06-20
  • Contact: Wang, Xicun

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46 | 5

1893年, 意大利化学家Biginelli首次利用芳香醛、乙酰乙酸乙酯和尿素三组分“一锅煮法”合成了3,4-二氢嘧啶-2(1H)-酮. 此类化合物具有良好的生物活性和反应活性, 对近几年来有关Biginelli 3,4-二氢嘧啶-2(1H)-酮的衍生化反应、Biginelli不对称合成和Biginelli反应在天然产物合成中的应用研究进行了综述.

关键词: 3,4-二氢嘧啶-2(1H)-酮, 不对称合成, 天然产物合成, Biginelli缩合反应

In 1893, Biginelli reported the first synthesis of 3,4-dihydropyrimidin-2(1H)-ones (DHPM) by a very simple one-pot condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate. It has been established that Biginelli-type dihydropyrimidinones present interesting pharmacological properties assiociated with good reactivities. In this article, the recent developments in the synthesis of DHPM derivatives, asymmetric Biginelli compounds and natural products using Biginelli reaction have been reviewed.

Key words: 3,4-dihydropyrimidin-2(1H)-one, asymmetric synthesis, natu-ral product synthes, Biginelli condensation reaction