[1]李 剑,王正兵,朱垧榕,等.Biginelli反应构建含炔基的二氢嘧啶衍生物的研究[J].常州大学学报(自然科学版),2019,31(05):9-15.[doi:10.3969/j.issn.2095-0411.2019.05.002]
　LI Jian,WANG Zhengbing,ZHU Shangrong,et al.Biginelli Reactions for the Construction of Alkynyl Substituted Dihydropyrimidinone[J].Journal of Changzhou University(Natural Science Edition),2019,31(05):9-15.[doi:10.3969/j.issn.2095-0411.2019.05.002]
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Biginelli反应构建含炔基的二氢嘧啶衍生物的研究()
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常州大学学报(自然科学版)[ISSN:2095-0411/CN:32-1822/N]

卷:
第31卷
期数:
2019年05期
页码:
9-15
栏目:
化学化工
出版日期:
2019-09-28

文章信息/Info

Title:
Biginelli Reactions for the Construction of Alkynyl Substituted Dihydropyrimidinone
文章编号:
2095-0411(2019)05-0009-07
作者:
李 剑; 王正兵; 朱垧榕; 胡曦文; 严生虎; 张 跃
(常州大学 制药与生命科学学院,江苏 常州 213164)
Author(s):
LI Jian;  WANG Zhengbing;  ZHU Shangrong;  HU Xiwen;  YAN Shenghu;  ZHANG Yue
(School of Pharmaceutical Engineering & Life Sciences, Changzhou University, Changzhou 213164, China)
关键词:
三组分反应;  Biginelli反应;  二氢嘧啶衍生物
Keywords:
three-component reaction;  Biginelli reaction;  dihydropyrimidinone derivatives
分类号:
O 621.3
DOI:
10.3969/j.issn.2095-0411.2019.05.002
文献标志码:
A
摘要:
研究了一种在铜催化下,以2-乙炔基苯甲醛衍生物、硫脲和β-酮酯为底物,通过Biginelli反应一步法合成含炔基的二氢嘧啶酮类衍生物的新方法,并用熔点、核磁1H NMR,13C NMR和高分辨质谱对化合物进行了结构表征。该方法原料简单易得,操作简便,合成效率高。通过对底物的适用性研究,发现芳基和开链的烷基炔烃苯甲醛都能很好地适用于该反应。
Abstract:
A simple and efficient one-pot synthesis of novel alkynyl substituted dihydropyrimidinones employing aldehyde, β-keto ester and sulfourea has been developed in the presence of copper catalyst. Various dihydropyrimidinone derivatives were obtained in moderate to good yields and all the target compounds were successfully prepared and confirmed with melting points, 1H NMR, 13C NMR and HRMS spectra. This reaction proceeds under mild reaction conditions with a high tolerance of a wide range of substrates including aryl and open chain alkyl.

参考文献/References:

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备注/Memo

备注/Memo:
收稿日期:2018-09-10。
基金项目:国家自然科学基金资助项目(21402013)。
作者简介:李剑(1980—),男,河南洛阳人,博士,副教授。E-mail: lijianchem@cczu.edu.cn
更新日期/Last Update: 2019-09-30