反应详情

To a microwave tube was added 2-chloro-N-methyl-5-(trifluoromethyl)pyrimidin-4-amine (112 mg, 0.53 mmol), 1-isopropyl-1H-pyrazol-4-amine (55 mg, 0.44 mmol), cesium carbonate (0.287 g, 0.88 mmol), XPhos (21 mg, 0.044 mmol), Pd2(dba)3 (20 mg, 0.02 mmol) and dioxane (2.5 mL). The tube was sealed and the reaction was irradiated in the microwave at 140° C. for 30 minutes. The reaction mixture was then filtered and concentrated. The crude product was purified by reverse phase HPLC to give N2-(1-isopropyl-1H-pyrazol-4-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine (22 mg, 16%). LCMS (Method A): [MH+]=301.1 at 3.2 min. 1H-NMR (DMSO): δ 9.43 (m, 2H), 8.08 (s, 1H), 7.89 (s, 1H), 7.54 (s, 1H), 6.96 (m, 2H), 4.43 (m, 1H), 2.92 (d, J=8.0, 3H), 1.39 (d, J=6.6, 6H).

1. customThe tube was sealed
2. customthe reaction was irradiated in the microwave at 140° C. for 30 minutes
3. filtrationThe reaction mixture was then filtered
4. concentrationconcentrated
5. customThe crude product was purified by reverse phase HPLC