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

[Display omitted] •N-phenethylquinazolin-4-amines were synthesized with excellent yields via silylation-amination mediated by hexamethyldisilazane (HMDS).•The protocol scope included phenethylamines with varied electronic and steric properties.•The enhanced efficiency of the silylation-amination method over the classical chlorination-amination procedure was demonstrated.•Method obtained in line with green chemistry principles for obtaining compounds with application in tuberculosis drug discovery programs. N-phenethylquinazolin-4-amines have emerged as potentialMycobacterium tuberculosiscytochromebdoxidase 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 accessN-phenethylquinazolin-4-amines via silylation-amination mediated by hexamethyldisilazane. The products were obtained with excellent yields (84–99%) under one-pot solvent-free conditions.