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1-cyclopropyl-7-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
80%
With triethylamine; In acetonitrile; for 16h;Reflux;
General procedure: A mixture of 7 (200mg, 0.754mmol), 12 (345mg, 1.5mmol), 11mL of anhydrous CH3CN and Et3N (0.47mL 3, 4mmol) was refluxed with drying tube. After 16h, the resulting suspension was filtered and the solid was washed first with CH3CN (3×3mL) and later with water (3×3mL). The solid was dried under high vacuum to afford pure fluoroquinolone 6 (263mg, 80percent) as an off white solid, mp 224?227°C. IR (cm?1) 3049.92; 3024.13; 2914.22; 2835.26; 1710.79; 1612.44; 1554.48; 1498.38. RMN 1H (300MHz, CDCl3) delta 15.10 (s, 1H); 8.74 (s, 1H); 7.92 (d; J=12.6Hz; 1H); 7.39 (d; J=8.4Hz; 1H); 7.28 (s, 1H), 6.68 (s, 1H); 4.52 (s, 2H); 3.89 (s, 6H); 3.76 (br t; J=5.7Hz; 2H); 3.58?3.47 (m, 1H); 2.97 (br t; J=5.4Hz; 2H); 1.42?1.12 (m, 4H). HRMS (ESI-TOF) m/z: [M+H]+ calculated for C24H23FN2O5 438.1591. Found: 438.1664.
Chemistry
Pharmaceutical Intermediates
Inhibitors/Agonists
Material Science
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120K+ Compounds
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