反应详情

Prepared according to procedure Y by stirring 4-chloro-7-fluoro-3-methyl-2-(4-methylpyridin-2-yl)quinoline (50 mg, 0.17 mmol), 6′-morpholino-1′,2,2′,3,5,6-hexahydrospiro[pyran-4,3′-pyrrolo[3,2-b]pyridine] (48.0 mg, 0.17 mmol), sodium tert-butoxide (33.5 mg, 0.35 mmol), XPhos precatalyst (26 mg, 0.035 mmol), and toluene (1.7 mL) at 90° C. for 18 h. Purification by reverse-phase HPLC (0-70% acetonitrile in water) gave 1′-(7-fluoro-3-methyl-2-(4-methyl-2-pyridinyl)-4-quinolinyl)-6′-(4-morpholinyl)-1′,2,2′,3,5,6-hexahydrospiro[pyran-4,3′-pyrrolo-[3,2-b]pyridine] as a yellow film. 1H NMR (400 MHz, chloroform-d) δ ppm 8.60 (1H, d, J=5.1 Hz), 7.87 (1H, dd, J=9.8, 2.5 Hz), 7.69-7.75 (2H, m), 7.59-7.61 (1H, m), 7.29-7.36 (1H, m), 7.23-7.27 (1H, m), 5.89 (1H, s), 4.14-4.21 (2H, m), 4.02 (2H, s), 3.70-3.81 (4H, m), 3.50-3.62 (2H, m), 2.95-3.09 (4H, m), 2.51 (4H, s), 2.45 (1H, s), 2.38 (3H, s), 1.81-1.90 (1H, m), 1.70-1.81 (1H, m). Mass Spectrum (ESI) m/e=526.2 (M+1).

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