Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China.
Org Biomol Chem. 2022 Aug 24;20(33):6654-6658. doi: 10.1039/d2ob01234k.
A catalyst-free method for the highly regioselective hydrated ring-opening and formylation of quinazolinones was developed. This reaction realized the direct arylation of two nitrogen atoms on quinazolinones and realized the regioselective ring-opening of quinazolinone and subsequent acylation of methyleneamine through the nucleophilic addition of a water molecule to an imine carbon atom. It showed reasonable functional group compatibility and provided one-pot access to a variety of -arylformyl derivatives in moderate to excellent yields.
开发了一种无催化剂的喹唑啉酮高区域选择性水合开环甲酰化方法。该反应实现了喹唑啉酮两个氮原子的直接芳基化，并通过水分子对亚胺碳原子的亲核加成，实现了喹唑啉酮的区域选择性开环和随后的亚甲胺酰化。它表现出合理的官能团相容性，并提供了一种一锅法以中等至优异的收率获得各种 -芳基甲酰基衍生物的方法。
