有机化学 ›› 2017, Vol. 37 ›› Issue (2): 514-519.DOI: 10.6023/cjoc201606030 上一篇    下一篇

研究简报

胃蛋白酶催化合成2,3-二氢喹唑啉-4(1H)-酮衍生物

谢宗波a,b, 张士国b, 姜国芳b, 梁萌b, 乐长高a,b   

  1. a 东华理工大学 江西省质谱科学与仪器2011协同创新中心 南昌 330013;
    b 东华理工大学应用化学系 南昌 330013
  • 收稿日期:2016-06-20 修回日期:2016-09-17 出版日期:2017-02-25 发布日期:2016-10-18
  • 通讯作者: 姜国芳, 乐长高 E-mail:zhgle@ecit.cn;gfjiang@ecit.cn
  • 基金资助:

    国家自然科学基金(Nos.21462001,21465002)、长江学者和创新团队发展计划(No.IRT13054)、江西省自然科学基金(No.20142BAB203008)资助项目.

Pepsin-Catalyzed Synthesis of 2,3-Dihydroquinazolin-4(1H)-one Derivatives

Xie Zongboa,b, Zhang Shiguob, Jiang Guofangb, Liang Mengb, Le Zhanggaoa,b   

  1. a Jiangxi 2011 Joint Center for the Innovative Mass Spectrometry and Instrumentation, East China University of Technology, Nanchang 330013;
    b Department of Applied Chemistry, East China University of Technology, Nanchang 330013
  • Received:2016-06-20 Revised:2016-09-17 Online:2017-02-25 Published:2016-10-18
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21462001, 21465002), the Program for Changjiang Scholars and Innovative Research Team in University (No. IRT13054), the Natural Science Foundation of Jiangxi Province (No. 20142BAB203008).

在乙醇溶剂中,考察了不同的酶对2-氨基苯甲酰胺与醛类物质环缩合反应的催化性能,确定胃蛋白酶为最佳的催化剂.然后对反应温度、酶用量、底物的物质的量比、反应时间等影响因素进行优化,确定了最佳的反应条件: 在65℃温度下,10 mg胃蛋白酶可以高效催化2-氨基苯甲酰胺与芳香醛及脂肪醛的反应,合成了一系列2,3-二氢喹唑啉-4(1H)-酮衍生物.

关键词: 2-氨基苯甲酰胺, 醛, 环缩合反应, 2,3-二氢喹唑啉-4(1H)-酮衍生物, 胃蛋白酶

The catalytic property of some hydrolases for the cyclocondensation of aldehydes with 2-aminobenzamide was researched in alcohol solvent, and pepsin was selected as the best catalyst. The reaction conditions were optimized through investigating the temperature, the enzyme loading, the ratio of substrates and the reaction time. Under the optimal conditions, 5 mg of pepsin could catalyze the cyclizing reaction of aldehydes with 2-aminobenzamide, and the corresponding 2,3-dihydroquinazolin-4(1H)-ones were successfully obtained in high yields.

Key words: 2-aminobenzamide, aldehyde, cyclocondensation, 2,3-dihydroquinazolin-4(1H)-ones, pepsin