Synthesis of N-phenethylquinazolin-4-amines via silylation-amination mediated by hexamethyldisilazane
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...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2022-01-01
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| Series: | Results in Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715622002582 |
| Summary: | 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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| ISSN: | 2211-7156 |