反应详情

Prepared according to Procedure X using palladium (II) acetate (2.1 mg, 9.17 μmol), XPhos (0.013 g, 0.028 mmol), 4-chloro-7-fluoro-3-methyl-2-(pyridin-2-yl)quinoline (0.050 g, 0.183 mmol), 3-amino-N-methyl-5-morpholinobenzamide (0.043 g, 0.183 mmol), potassium carbonate (0.063 g, 0.458 mmol), and tert-butanol (1 mL). Purification using column chromatography (silica; 0-5% methanol in DCM) afforded 3-((7-fluoro-3-methyl-2-(2-pyridinyl)-4-quinolinyl)amino)-N-methyl-5-(4-morpholinyl)benzamide as a yellow amorphous solid. 1H NMR (400 MHz, CHLOROFORM-d) δ ppm 8.70-8.76 (1H, m), 7.80-7.95 (3H, m), 7.72-7.79 (1H, m), 7.35-7.44 (1H, m), 7.14-7.23 (1H, m), 6.88-6.96 (1H, m), 6.53-6.59 (1H, m), 6.36-6.43 (1H, m), 6.21-6.32 (1H, m), 6.15 (1H, br. s.), 3.76-3.84 (4H, m), 3.07-3.14 (4H, m), 2.93 (3H, d, J=4.7 Hz), 2.33 (3H, s). Mass Spectrum (ESI) m/e=472.1 (M+1).

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