反应详情

Prepared according to procedure Y by using 6′-morpholino-1′,2,2′,3,5,6-hexahydrospiro[pyran-4,3′-pyrrolo[3,2-b]pyridine] (70 mg, 0.254 mmol), 4-chloro-3-methyl-2-(pyridin-2-yl)-1,8-naphthyridine (65.0 mg, 0.25 mmol), sodium tert-butoxide (48.9 mg, 0.51 mmol) and XPhos precatalyst (18.7 mg, 0.025 mmol) in toluene (5 mL) for 2 h at 100° C. Purification by reverse phase HPLC (10 to 60% acetonitrile in water) gave 1′-(3-methyl-2-(pyridin-2-yl)-1,8-naphthyridin-4-yl)-6′-morpholino-1′,2,2′,3,5,6-hexahydrospiro[pyran-4,3′-pyrrolo[3,2-b]pyridine]. 1H NMR (400 MHz, chloroform-d) δ ppm 9.13 (1H, dd, J=4.1, 2.0 Hz), 8.72 (1H, ddd, J=4.8, 1.8, 1.0 Hz), 8.19 (1H, dt, J=7.8, 1.2 Hz), 8.13 (1H, dd, J=8.4, 2.0 Hz), 7.93 (1H, td, J=7.7, 1.8 Hz), 7.64 (1H, d, J=2.3 Hz), 7.39-7.47 (2H, m), 5.82 (1H, d, J=2.3 Hz), 4.13-4.20 (2H, m), 4.08 (1H, d, J=9.8 Hz), 3.97 (1H, d, J=9.6 Hz), 3.72-3.78 (4H, m), 3.55-3.62 (2H, m), 2.95-3.04 (4H, m), 2.51 (3H, s), 2.20-2.35 (2H, m), 1.74-1.87 (2H, m). Mass Spectrum (ESI) m/e=495.2 (M+1).

1. customPrepared
2. customfor 2 h
3. customat 100° C
4. customPurification by reverse phase HPLC (10 to 60% acetonitrile in water)