反应详情

温度

80 °C

To a solution of (4-chloro-3-trifluoromethyl-phenyl)-[5-(2-methanesulfonyl-pyrimidin-4-yloxy)-1H-benzimidazol-2-yl]-amine (Step B, 120 mg, 0.2 mmol, 1.0 eq.) in anhydrous THF (4 mL) was added 1 mL of 2 M CH3NH2 in THF (2 mmol, 10 eq). The solution was heated to 80° C. for 1 h. The THF was removed under reduced pressure and the crude was purified by column chromatography (0-10% MeOH/CH2Cl2 with 1% NH4OH) to yield pure (4-chloro-3-trifluoromethyl-phenyl)-[5-(2-methylamino-pyrimidin-4-yloxy)-1H-benzimidazol-2-yl]-amine. MS m/z=435.1 (M+H)+; MW Calc'd for C19H14ClF3N6O: 434.09.

1. customThe THF was removed under reduced pressure
2. customthe crude was purified by column chromatography (0-10% MeOH/CH2Cl2 with 1% NH4OH)