Synthesis of 2,3-dihydroquinazolin-4(1H)-ones catalyzed by α-chymotrypsin

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• 作者：Shi-Guo Zhang^b ; Zong-Bo Xie^a ; ^b ; ^{zbxie@ecit.cn} ; Lian-Sheng Liu^b ; Meng Liang^b ; Zhang-Gao Le^a ; ^b ; ^{zhgle@ecit.cn}
• 关键词：2 ; 3-Dihydroquinazolin-4(1H)-ones ; α-Chymotrypsin ; Cyclocondensation ; Biocatalysis ; 2-Aminobenzamides
• 刊名：Chinese Chemical Letters
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：28
• 期：1
• 页码：101-104
• 全文大小：295 K
• 卷排序：28

文摘

We discovered that α-chymotrypsin has a promiscuous ability to catalyze the cyclocondensation of aromatic and aliphatic aldehydes with 2-aminobenzamides to afford the corresponding 2,3-dihydroquinazolin-4(1H)-ones successfully in high yields (90%–98%) under alcohol solvent. The catalytic activity of α-chymotrypsin was evaluated through investigating the temperature, the enzyme loading and the ratio of substrates in the enzyme-catalyzed reactions. The present method proves to be efficient and environmentally friendly in terms of short reaction time, high yield, green catalyst and the clean products obtained without further purification processes.