反应详情

温度

100 °C

To a de-gassed mixture of 5-chloro-2-(6-methoxy-3-trifluoromethyl-pyridin-2-yl)-[1,8]naphthyridine (68 mg, 0.2 mmol), cesium carbonate (98 mg, 0.3 mmol), 2-amino-5-trifluoromethylpyrimidine (37 mg, 0.22 mmol) in dioxane (5 mL) under nitrogen, add Pd2 dba3 (12 mg) and xantphos (8 mg). Stir the mixture at 100° C. for 14 hours, cool, add water (20 mL) and extract with EtOAc. Dry the combined extracts over Na2SO4, and concentrate under vacuum. Purify by chromatography eluting with DCM/MeOH/ammonium hydroxide mixture to give the title compound. 1H NMR δ (CDCl3) 9.14 (1H, d), 8.81 (2H, s), 8.56 (2H, d), 8.40 (1H, brs), 7.99 (2H, dd), 7.26 (1H, s), 6.92 (1H, d), 4.01 (3H, s). The IC50 determined as described in Example 6 is less than 1 micromolar.

1. temperaturecool
2. extractionextract with EtOAc
3. dry with materialDry the combined extracts over Na2SO4
4. concentrationconcentrate under vacuum
5. customPurify by chromatography
6. washeluting with DCM/MeOH/ammonium hydroxide mixture