反应详情

To a solution of 4-(4-chloro-6-methoxy-3-nitroquinolin-7-yl)-3,5-dimethylisoxazole (for a preparation, see Intermediate 8) (1 g, 3.00 mmol) in 1,4-dioxane (6.5 mL) was added (R)-1-(pyridin-2-yl)ethanamine (0.549 g, 4.49 mmol) and the mixture stirred at room temperature for 5 h. A further portion of (R)-1-(pyridin-2-yl)ethanamine (0.255 g, 2.25 mmol) was added and the mixture stirred at room temperature overnight. The solvent was removed under reduced pressure and the residue purified by chromatography (50 g column, cyclohexane/EtOAc gradient) to give 7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-3-nitro-N—((R)-1-(pyridin-2-yl)ethyl)quinolin-4-amine (1.15 g, 2.74 mmol, 92% yield) as an orange solid. LCMS: (Formate, 2 min), Rt 0.98 mins, MH+ 420.

1. stirringthe mixture stirred at room temperature overnight
2. customThe solvent was removed under reduced pressure
3. customthe residue purified by chromatography (50 g column, cyclohexane/EtOAc gradient)