Work

PEG‐400 Mediated N ‐(Alkyl)Arylation for the Synthesis of Medicinally Relevant 4‐Aminoquinazolines

Year: 2025

Type: article

Abstract: 4‐Aminoquinazolines are an important class of heterocyclic aromatic compounds with extensive applications in pharmaceutical synthesis and materials science. Herein, we present a rapid, cost‐effective, and efficient approach for N‐(alkyl)arylation of 4‐chloroquinazolines using PEG‐400 as a green solvent alternative in both microwave and conventional heating reactors. These methodologies demonstrate broad compatibility with various substituted amines, yielding favorable outcomes. The developed approach enabled the synthesis of Verubulin, a promising antineoplastic agent for treating several types of cancer, alongside a novel drug analogue, highlighting its potential utility in sustainable drug synthesis and discovery.

Source: ChemistrySelect

DOI: 10.1002/slct.202405163

Authors: Gabriel de Paula Bueno, Luiz Vinícius Santos de Oliveira, Giovanna Preterotto Lourençon, Victor Hugo Catricala Fernandes, Leandro Alves Bozzini, Giuliano Cesar Clososki

Institution: Universidade de São Paulo

Language: English

Topic: Quinazolinone synthesis and applications

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: hybrid

Estimated APC paid: $3,880

Funders: Fundação de Amparo à Pesquisa do Estado de São Paulo, Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Conselho Nacional de Desenvolvimento Científico e Tecnológico