Efficient -arylation of 4-chloroquinazolines en route to novel 4-anilinoquinazolines as potential anticancer agents.

Beilstein J Org Chem

Núcleo de Pesquisas em Produtos Naturais e Sintéticos, Departamento de Ciências BioMoleculares, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Av. do Café s/n, Ribeirão Preto-SP 14040-903, Brazil.

Published: December 2021

Microwave-mediated -arylation of 4-chloroquinazolines in THF/HO rapidly and efficiently afforded a library of novel 6-halo-2-phenyl-substituted 4-anilinoquinazolines. The methodology was compatible with numerous , , and -substituted -methylanilines as well as substituted anilines and furnished the corresponding 4-anilinoquinazolines in good yields. Preliminary screening of the synthesized compounds against tumor cells (HCT-116 and T98G) showed promising antiproliferative properties.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8712970PMC
http://dx.doi.org/10.3762/bjoc.17.206DOI Listing

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Efficient -arylation of 4-chloroquinazolines en route to novel 4-anilinoquinazolines as potential anticancer agents.

Beilstein J Org Chem

December 2021

Núcleo de Pesquisas em Produtos Naturais e Sintéticos, Departamento de Ciências BioMoleculares, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Av. do Café s/n, Ribeirão Preto-SP 14040-903, Brazil.

Microwave-mediated -arylation of 4-chloroquinazolines in THF/HO rapidly and efficiently afforded a library of novel 6-halo-2-phenyl-substituted 4-anilinoquinazolines. The methodology was compatible with numerous , , and -substituted -methylanilines as well as substituted anilines and furnished the corresponding 4-anilinoquinazolines in good yields. Preliminary screening of the synthesized compounds against tumor cells (HCT-116 and T98G) showed promising antiproliferative properties.

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