反应详情

温度

50 °C

3-(2-Methoxy-2-phenylacetyl)dihydro-2H-pyran-4(3H)-one (100 mg, 0.40 mmol), 1-(4-(2-methyl-1H-imidazol-1-yl)phenyl)guanidine (Example 41c) (87 mg, 0.40 mmol) and potassium carbonate (55.7 mg, 0.40 mmol) was slurrified in EtOH (4 mL) and heated to 50° C. for 15 h. DCM and water were added. The organic phase was separated, dried with MgSO4 concentrated and purified by preparative HPLC yielding 4-(methoxy(phenyl)methyl)-N-(4-(2-methyl-1H-imidazol-1-yl)phenyl)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-amine (10.0 mg, 5.7%). MS (ES+) m/z 428.1 (M+H)+

1. customThe organic phase was separated
2. dry with materialdried with MgSO4
3. concentrationconcentrated
4. custompurified by preparative HPLC