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

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Autor(es):
Bueno, Gabriel de Paula ; de Oliveira, Luiz Vinicius Santos ; Lourencon, Giovanna Preterotto ; Fernandes, Victor Hugo Catricala ; Bozzini, Leandro Alves ; Clososki, Giuliano Cesar
Número total de Autores: 6
Tipo de documento: Artigo Científico
Fonte: CHEMISTRYSELECT; v. 10, n. 15, p. 7-pg., 2025-04-01.
Resumo

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. (AU)

Processo FAPESP: 22/05327-7 - Explorando o espaço químico medicinal de aromáticos com ferramentas sintéticas altamente seletivas
Beneficiário:Giuliano Cesar Clososki
Modalidade de apoio: Auxílio à Pesquisa - Regular