胃蛋白酶非天然催化活性的新用途:高效合成四氢喹唑啉  

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

作　　者：姜国芳[1] 卢粤 李红霞 胡智宇 朱潇 谢宗波[1] 乐长高[1] Jiang Guofang;Lu Yue;Li Hongxia;Hu Zhiyu;Zhu Xiao;Xie Zongbo;Le Zhanggao(Jiangxi Province Key Laboratory of Synthetic Chemistry,School of Chemistry,Biology and Material Science,East China University of Technology,Nanchang,Jiangxi 330013)

机构地区：[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

出　　处：《有机化学》2020年第9期2827-2835,共9页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21462001);江西省科技(No.20161BCB24006)资助项目。

摘　　要：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.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.

关 键 词：胃蛋白酶 非天然催化活性 四氢喹唑啉 生物催化 

分 类 号：O626[理学—有机化学]