Abstract

4-aminoquinazoline derivatives exhibit unique physiological activities, including antitumor, anti-inflammatory, and antibacterial biological activities. Afatinib (BIBW-2992), the representative tyrosine kinase inhibitor, has been developed for the treatment of non-small cell lung cancer. Following our expanded medical chemistry research program, we report a novel 4-aminoquinazoline derivative named JSLN-P (1), (5S)-5-[(2-(5-bromo-2-methoxyphenyl) quinazolin-4-ylamino)methyl]-3-(3-fluoro-4-morpholino phenyl) oxazolidin-2-one, aimed for developing new drugs with antiglioma properties. The title compound JSLN-P (1) was successfully synthesized by amination approaches following benzylamination and oxazolone cyclization, further condensation with 4-(4-bromo-2-fluorophenyl) morpholine, reduction in debenzylation and halogenated amination of quinazolin. The structure of JSLN-P (1) was confirmed by 1H and 13C nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS).

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