反应详情

Following the procedure described for Intermediate 13, Intermediate 15 (470 mg, 1.1 mmol) and TFA (3 mL) in DCM (6 mL) afforded (S)-1-{7-fluoro-8-methyl-2-[4-(pyrazin-2-yl)piperazin-1-yl]quinolin-3-yl}ethanamine as a white foam, which was used in the next step without any further purification. Following the procedure described for Example 5, (S)-1-{7-fluoro-8-methyl-2-[4-(pyrazin-2-yl)piperazin-1-yl]quinolin-3-yl}-ethanamine (60 mg, 0.16 mmol), 4-chloropyrido[3,2-d]pyrimidine (33 mg, 0.19 mmol) and DIPEA (0.14 mL, 0.8 mmol) in NMP (1.2 mL) afforded the title compound (37 mg, 46%) as a brown solid. δH (DMSO-d6) 8.95-8.89 (2H, m), 8.55 (2H, d, J 14.1 Hz), 8.45 (1H, d, J 1.5 Hz), 8.19-8.14 (2H, m), 7.93-7.88 (2H, m), 7.74 (1H, dd, J 8.9, 6.3 Hz), 7.33 (1H, t, J 9.1 Hz), 5.98-5.90 (1H, m), 3.96-3.87 (2H, m), 3.87-3.75 (4H, m), 3.33-3.25 (2H, m), 2.58 (3H, d, J 2.3 Hz), 1.68 (3H, d, J 6.7 Hz). LCMS (ES+) 496 (M+H)+, RT 4.07 minutes (Method 4).

1. customwas used in the next step without any further purification