反应详情

To a stirred solution of 4-chloro-2-(3,5-difluorophenyl)-3-methyl-1,8-naphthyridine (40 mg, 0.14 mmol), 4-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]-pyridin-6-yl)morpholine (32 mg, 0.14 mmol) and XPhos precatalyst (10 mg, 0.014 mmol) in toluene (4 mL) was added sodium tert-butoxide (26 mg, 0.27 mmol) and the reaction was heated at reflux for 2 h. Purification by reverse phase HPLC (10 to 60% acetonitrile in water) gave 2-(3,5-difluorophenyl)-N-(2,5-di-4-morpholinylphenyl)-3-methyl-1,8-naphthyridin-4-amine. H NMR (400 MHz, chloroform-d) δ ppm 9.10 (1H, dd, J=4.1, 2.0 Hz), 8.26 (1H, dd, J=8.4, 2.0 Hz), 7.40 (1H, dd, J=8.4, 4.1 Hz), 7.21-7.31 (2H, m), 7.13 (1H, d, J=8.6 Hz), 6.91-6.93 (1H, m), 6.48 (1H, dd, J=8.7, 2.6 Hz), 5.96 (1H, d, J=2.7 Hz), 3.91 (4H, t, J=4.6 Hz), 3.71-3.73 (4H, m), 3.05 (4H, br s), 2.87-2.90 (4H, m), 2.38 (3H, s). Mass Spectrum (ESI) m/e=518.2 (M+1).

1. temperaturethe reaction was heated
2. temperatureat reflux for 2 h
3. customPurification by reverse phase HPLC (10 to 60% acetonitrile in water)