反应详情

温度

90 °C

The mixture of 1-bromo-3-(3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine-7-yl)imidazo[1,5-a]pyrazin-8-amine (200 mg, 0.497 mmol), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide (194.54 mg, 0.497 mmol), Pd(dppf)Cl2 (18.3 mg, 0.025 mmol) and K2CO3 (137.26 mg, 0.995 mmol) in dioxane/H2O (5 mL/0.5 mL) was stirred at 90° C. for 2 h under nitrogen atmosphere. Remove the solvent in vacuo. The mixture was treated with ethyl acetate and water, the organic layer was separated, dried over sodium sulfate, filtered and the filtrate was concentrated. The residue was purified by preparative HPLC separation to give 4-(8-amino-3-(3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-7-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide (0.16 g, yield 50%).

1. customRemove the solvent in vacuo
2. additionThe mixture was treated with ethyl acetate and water
3. customthe organic layer was separated
4. dry with materialdried over sodium sulfate
5. filtrationfiltered
6. concentrationthe filtrate was concentrated
7. customThe residue was purified by preparative HPLC separation