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

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.

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Publication Details

Journal
ChemistrySelect
Published
2025-04-01
DOI
https://doi.org/10.1002/slct.202405163
Citations
3
Primary Topic
Quinazolinone synthesis and applications
Type
article
Field-Weighted Citation Impact
2.81

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article

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

Leandro A. Bozzini, Victor Hugo Catricala Fernandes, Luiz Henrique Bastos da Silva de Oliveira, Gabriel de P. Bueno et al.
3 citations
ChemistrySelect
Quinazolinone synthesis and applications
2.81
article

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

Leandro A. Bozzini, Victor Hugo Catricala Fernandes, Luiz Henrique Bastos da Silva de Oliveira, Gabriel de P. Bueno, Giovanna Preterotto Lourençon, Giuliano Cesar Clososki
article en
3 citations

Abstract

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.

ChemistrySelectVol. 10(15)
Universidade de São Paulo (BR), SUPERA Park of Innovation and Technology of Ribeirão Preto (BR)
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
Openalex Percentile: Top 11%
Quinazolinone synthesis and applications
2.81
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PEG‐400 Mediated <i>N</i> ‐(Alkyl)Arylation for the Synthesis of Medicinally Relevant 4‐Aminoquinazolines — Leandro A. Bozzini, Victor Hugo Catricala Fernandes, et al. · ChemistrySelect (2025) | TGRS Research Map | TGRS