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Beilstein-Institut, Beilstein Journal of Organic Chemistry, (17), p. 2968-2975, 2021

DOI: 10.3762/bjoc.17.206

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

Journal article published in 2021 by Rodolfo H. V. Nishimura ORCID, Thiago dos Santos ORCID, Valter E. Murie ORCID, Luciana C. Furtado ORCID, Leticia V. Costa-Lotufo ORCID, Giuliano C. Clososki ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

Microwave-mediated N-arylation of 4-chloroquinazolines in THF/H2O rapidly and efficiently afforded a library of novel 6-halo-2-phenyl-substituted 4-anilinoquinazolines. The methodology was compatible with numerous ortho-, meta-, and para-substituted N-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.