反应详情

Prepared according to procedure Y using 4-chloro-2-(3,5-difluorophenyl)-3-methyl-1,7-naphthyridine (40 mg, 0.138 mmol), 4-(3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-6-yl)morpholine (32.1 mg, 0.138 mmol), sodium tert-butoxide (26.4 mg, 0.275 mmol) and XPhos precatalyst (10.4 mg, 0.014 mmol) in toluene (4 mL) for 2 hours at 110° C. Purification by reverse phase HPLC (10 to 60% acetonitrile in water) gave 2-(3,5-difluorophenyl)-4-(3,3-dimethyl-6-(4-morpholinyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-3-methyl-1,7-naphthyridine. 1H NMR (400 MHz, chloroform-d) δ ppm 9.59 (1H, d, J=1.0 Hz), 8.57 (1H, d, J=5.9 Hz), 7.69 (1H, d, J=2.3 Hz), 7.51 (1H, dd, J=5.9, 1.0 Hz), 7.15-7.22 (2H, m), 6.94-7.01 (1H, m), 5.82 (1H, d, J=2.3 Hz), 4.13-4.23 (2H, m), 3.71-3.81 (4H, m), 3.59 (2H, tt, J=11.4, 2.8 Hz), 2.95-3.07 (4H, m), 2.29-2.45 (5H, m), 1.71-1.92 (2H, m). Mass Spectrum (ESI) m/e=488.2 (M+1).

1. customPrepared
2. customfor 2 hours
3. customat 110° C
4. customPurification by reverse phase HPLC (10 to 60% acetonitrile in water)