反应详情

温度

100 °C

To a de-gassed mixture of 3-[3-(trifluoromethyl)pyridin-2-yl]pyrido[2,3-b]pyrazin-8-amine (72 mg, 0.25 mmol), cesium carbonate (162 mg, 0.5 mmol), 2-amino-trifluoromethyl pyridine (45 mg, 0.25 mmol) in dioxane (5 mL) under nitrogen, add Pd2dba3 (11 mg) and xantphos (7 mg). Stir the mixture at 100° C. for 3 hours, cool, add water (10 mL) and extract with EtOAc. Dry over Na2SO4, concentrate under vacuum. Purify by chromatography eluting with dichloromethane/methanol/ammonium hydroxide mixture to give the title compound. MS 437 (M+1). 1H NMR δ (CDCl3) 9.42 (1H, s), 9.28 (1H, s), 9.11 (1H, d), 8.95 (1H, d), 8.90 (1H, d), 8.72 (1H, s), 8.25 (1H, d), 7.89 (1H, d), 7.61 (1H,dd), 7.13 (1H, d).

1. temperaturecool
2. extractionextract with EtOAc
3. dry with materialDry over Na2SO4
4. concentrationconcentrate under vacuum
5. customPurify by chromatography
6. washeluting with dichloromethane/methanol/ammonium hydroxide mixture