Catalyst-free highly regioselective hydrated ring-opening and formylation of quinazolinones†
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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