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Updated: Apr 18, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Three-component reaction toward polyannulated quinazolinones, benzoxazinones, and benzothiazinones
Denis Kröger1, Torben Schlüter, Malte Fischer
1Carl von Ossietzky Universität Oldenburg Fakultät für Mathematik und Naturwissenschaften Institut für Chemie Carl-von-Ossietzky-Strasse 9-11, 26129 Oldenburg, Deutschland.
Abstract:
An efficient conversion of readily accessible cyclic imines with acid chlorides, that are able to take part in nucleophilic aromatic substitution (SNAr) reactions is realized in a new three-component, one-pot reaction, giving at least tricyclic annulated quinazolinones, benzoxazinones, and benzothiazinones as a result of the employed nitrogen, oxygen, or sulfur nucleophiles, respectively. Especially in the case of quinazolinones, this convenient strategy enables the access to heterocycles of heightened diversity, which offer the development of efficient derivatizations of the elaborated heterocyclic scaffolds. In a subsequent Heck or Ullmann cyclization, further annulations to the mentioned quinazolinones can be carried out.
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