反应详情

Prepared according to Procedure X by stirring palladium (II) acetate (0.3 mg, 1.417 μmol), XPhos (2.0 mg, 4.25 μmol), 1-(4-chloro-7-fluoro-3-methylquinolin-2-yl)pyrrolidin-2-one (0.020 g, 0.071 mmol), N-(3-amino-5-morpholinophenyl)-acetamide (0.020 g, 0.085 mmol), potassium carbonate (0.024 g, 0.177 mmol), and tert-butanol (0.5 mL) at 110° C. for 30 minutes. Purification by reverse-phase HPLC (0-70% acetonitrile in water) afforded N-(3-((7-fluoro-3-methyl-2-(2-oxo-1-pyrrolidinyl)-4-quinolinyl)amino)-5-(4-morpholinyl)phenyl)acetamide as a yellow amorphous solid. 1H NMR (500 MHz, CHLOROFORM-d) δ ppm 7.80 (1H, dd, J=8.8, 7.3 Hz), 7.51-7.61 (1H, m), 7.45 (1H, br. s.), 7.08-7.19 (1H, m), 6.79-6.99 (1H, m), 6.37 (1H, br. s.), 6.25 (1H, br. s.), 6.05 (1H, br. s.), 4.13 (2H, d, J=7.1 Hz), 3.77 (4H, t, J=4.9 Hz), 3.08 (4H, t, J=4.9 Hz), 2.63 (2H, t, J=8.1 Hz), 2.23-2.36 (2H, m), 2.13 (3H, s), 2.06-2.10 (3H, m). Mass Spectrum (ESI) m/e=478.2 (M+1).

1. customPrepared
2. customPurification by reverse-phase HPLC (0-70% acetonitrile in water)