2-((6,7-Dimethoxy-4-oxo-3-(4-(trifluoromethyl)phenethyl)-3,4-dihydroquinazolin-2-yl)thio)-N-(4-ethylphenyl)butanamide

2-({3-[2-(1-cyclohexen-1-yl)ethyl]-6,7-dimethoxy-4-oxo-3,4-dihydro-2-quinazolinyl}sulfanyl)-N-(4-ethylphenyl)butanamide (K284-6111; K284), the representative CHI3L1 inhibitor, has interesting biological activities, including anti-cancer and anti-inflammatory effects on neuroinflammation. Following our hit-to-lead program, we report the most active novel derivative, named CBJL-025, 2-((6,7-dimethoxy-4-oxo-3-(4-(trifluoromethyl)phenethyl)-3,4-dihydroquinazolin-2-yl)thio)-N-(4-ethylphenyl)butanamide. The title compound, CBJL-025, was successfully synthesized by S-alkylation of the p-trifluoromethyl phenethyl group possessing quinazoline and the corresponding bromide. The structure of CBJL-025 was confirmed by 1H and 13C nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS).