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

Microwave-mediated -arylation of 4-chloroquinazolines in THF/H O 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...

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Bibliographic Details
Published in:Beilstein journal of organic chemistry 2021-12, Vol.17 (1), p.2968-2975
Main Authors: Nishimura, Rodolfo H V, Dos Santos, Thiago, Murie, Valter E, Furtado, Luciana C, Costa-Lotufo, Leticia V, Clososki, Giuliano C
Format: Article
Language:English
Subjects:
4-anilinoquinazoline
4-chloroquinazoline
anticancer agents
Chemistry
Full Research Paper
microwave irradiation
n-arylation
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Summary:Microwave-mediated -arylation of 4-chloroquinazolines in THF/H O 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.
ISSN:1860-5397
1860-5397
DOI:10.3762/bjoc.17.206