反应详情

6-[5-(3-Fluoropyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-N-methyl-N-phenyl-[1,3,5]triazine-2,4-diamine (prepared in an analogous manner to Example 482, 50 mg, 0.137 mmol), 1-cyclopropylmethanamine (24 μL, 0.274 mmol) and potassium carbonate (57 mg, 0.411 mmol) were suspended in anhydrous DMF (2 mL) in a sealed tube at room temperature under nitrogen. The reaction mixture was stirred at 90 C for 3 h and then at 100 C for 18 h. The mixture was diluted with DCM (10 mL) and then washed with saturated aq. ammonium chloride (3×5 mL) and then brine (5 mL). The organic layer was dried over sodium sulfate and evaporated under vacuum. The crude residue was purified by flash chromatography (0-1% (7M ammonia in MeOH) in DCM) to afford the title compound (25 mg, 44%).

1. waitat 100 C for 18 h
2. washwashed with saturated aq. ammonium chloride (3×5 mL)
3. dry with materialThe organic layer was dried over sodium sulfate
4. customevaporated under vacuum
5. customThe crude residue was purified by flash chromatography (0-1% (7M ammonia in MeOH) in DCM)