反应详情

温度

100 °C

To a microwave vial was added sodium tert-butoxide (0.035 g, 0.37 mmol), ruphos (8.6 mg, 0.018 mmol), 4-chloro-7-fluoro-3-methyl-2-(pyridin-2-yl)-quinoline (0.053 g, 0.19 mmol), 2,2-dimethyl-6′-morpholinospiro[[1,3]dioxane-5,3′-indoline] (0.056 g, 0.18 mmol), and XPhos pre-catalyst (0.014 g, 0.018 mmol) in toluene (1.2 mL). The suspension was deoxygenated with argon for 5 min and stirred at 100° C. for 90 min under microwave irradiation. Purification by column chromatography (eluting with a gradient of 10-60% EtOAc in hexanes) gave 1′-(7-fluoro-3-methyl-2-(pyridin-2-yl)quinolin-4-yl)-2,2-dimethyl-6′-morpholinospiro[[1,3]dioxane-5,3′-indoline] as a yellow solid. Mass Spectrum (ESI) m/e=541.3 (M+1).

1. customThe suspension was deoxygenated with argon for 5 min
2. customPurification by column chromatography (
3. washeluting with a gradient of 10-60% EtOAc in hexanes)