在通往新型4-苯胺基喹唑啉类潜在抗癌药物的过程中4-氯喹唑啉的高效芳基化反应
Efficient -arylation of 4-chloroquinazolines en route to novel 4-anilinoquinazolines as potential anticancer agents.
作者信息
Nishimura Rodolfo H V, Dos Santos Thiago, Murie Valter E, Furtado Luciana C, Costa-Lotufo Leticia V, Clososki Giuliano C
机构信息
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.
Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto-SP, Universidade de São Paulo, Av. dos Bandeirantes 3900, Ribeirão Preto-SP 14090-901, Brazil.
出版信息
Beilstein J Org Chem. 2021 Dec 22;17:2968-2975. doi: 10.3762/bjoc.17.206. eCollection 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.
在四氢呋喃/水体系中，微波介导的4-氯喹唑啉的芳基化反应能够快速、高效地构建一系列新型的6-卤代-2-苯基取代的4-苯胺基喹唑啉文库。该方法适用于多种邻位、间位和对位取代的甲基苯胺以及取代苯胺，能以良好的产率得到相应的4-苯胺基喹唑啉。对合成化合物针对肿瘤细胞（HCT-116和T98G）进行的初步筛选显示出有前景的抗增殖特性。
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