Synthesis of N-phenethylquinazolin-4-amines via silylation-amination mediated by hexamethyldisilazane

Autor: Guilherme Arraché Gonçalves, Flávio Castro do Nascimento, Sidnei Moura e Silva, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Results in Chemistry, Vol 4, Iss , Pp 100539- (2022)
Druh dokumentu: article
ISSN: 2211-7156
DOI: 10.1016/j.rechem.2022.100539
Popis: N-phenethylquinazolin-4-amines have emerged as potential Mycobacterium tuberculosis cytochrome bd oxidase inhibitors and attractive scaffolds in tuberculosis drug discovery programs. The classical two-step strategy of chlorination-amination to synthesize such structures presents several operational issues accompanied by variable results. This work reports an efficient one-pot protocol to access N-phenethylquinazolin-4-amines via silylation-amination mediated by hexamethyldisilazane. The products were obtained with excellent yields (84–99%) under one-pot solvent-free conditions.
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