有机化学 ›› 2020, Vol. 40 ›› Issue (9): 2827-2835.DOI: 10.6023/cjoc202006006 上一篇    下一篇

研究论文

胃蛋白酶非天然催化活性的新用途:高效合成四氢喹唑啉

姜国芳, 卢粤, 李红霞, 胡智宇, 朱潇, 谢宗波, 乐长高   

  1. 东华理工大学化学生物与材料科学学院 江西省合成化学重点实验室 江西南昌 330013
  • 收稿日期:2020-06-05 修回日期:2020-06-12 发布日期:2020-06-28
  • 通讯作者: 谢宗波, 乐长高 E-mail:zbxie@ecut.edu.cn;zhgLe@ecut.edu.cn
  • 基金资助:
    国家自然科学基金(No.21462001)、江西省科技(No.20161BCB24006)资助项目.

New Use of Non-natural Catalytic Activity of Pepsin: Highly Efficient Synthesis of Tetrahydroquinazolines

Jiang Guofang, Lu Yue, Li Hongxia, Hu Zhiyu, Zhu Xiao, Xie Zongbo, Le Zhanggao   

  1. Jiangxi Province Key Laboratory of Synthetic Chemistry, School of Chemistry, Biology and Material Science, East China University of Technology, Nanchang, Jiangxi 330013
  • Received:2020-06-05 Revised:2020-06-12 Published:2020-06-28
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21462001), and the Science and Technology Projects of Jiangxi Province (No. 20161BCB24006).

猪胃粘膜蛋白酶具有催化芳香胺和2-氨基苯甲醛环化缩合反应的能力,在甲醇水溶液中,以良好的收率(41%~95%)合成了一系列四氢喹唑啉类化合物.通过优化酶促反应的溶剂、温度、酶用量和底物比例来提高胃蛋白酶的催化活性.该方法可作为四氢喹唑啉衍生物化学合成的替代方法,也进一步拓展了胃蛋白酶非天然催化活性的应用范围.

关键词: 胃蛋白酶, 非天然催化活性, 四氢喹唑啉, 生物催化

Pepsin from porcine gastric mucosa has a non-natural ability to catalyze the cyclocondensation of aromatic amines and 2-aminobenzaldehyde. The corresponding tetrahydroquinazolines were obtained in good yields (41%~95%) in aqueous methanol solution. The catalytic activity of pepsin was evaluated by investigating solvent, temperature, enzyme loading, and substrate ratio in the enzyme-catalyzed reaction. Herein, a potential biocatalytic approach as an alternative to chemical synthesis for tetrahydroquinazoline derivatives was proposed.

Key words: pepsin, non-natural catalytic activity, tetrahydroquinazoline, biocatalysis