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-trifluoromethylpyridine (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, concentrate under vacuum. Purify by chromatography eluting with DCM/MeOH/ammonium hydroxide mixture to give the title compound. 1H NMR δ (CDCl3) 9.01 (1H, brs), 8.59-8.62 (2H, m), 7.98-8.01 (2H, m), 7.91-7.84 (2H, m), 7.23-7.26 (2H, m), 6.90 (1H, d), 3.99 (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