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Updated: Sep 2, 2025

Preparation of Contiguous Bisaziridines for Regioselective Ring-Opening Reactions
Published on: July 28, 2022
Catalyst-free highly regioselective hydrated ring-opening and formylation of quinazolinones
Xianglin Yu1, Zhiliang Tang1, Kun He1
1Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China. jinyi@ynu.edu.cn.
Abstract:
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 N-arylformyl derivatives in moderate to excellent yields.
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