Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (9): 2827-2835.DOI: 10.6023/cjoc202006006 Previous Articles     Next Articles


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;
  • 基金资助:

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).

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