反应详情

温度

130 °C

16 mg of 5-bromo-2-trifluoromethyl-pyridine, 50 mg of cesium carbonate and 10 mg of copper(II) oxide were added to an N-methylpyrrolidinone (1 ml) solution of 21 mg of 5-(2-fluorophenoxy)-6-hydroxy-2-pyrazin-2-yl-1H-benzimidazole obtained in Example 251 (step 1), and the reaction liquid was stirred at 130° C. for 5 hours. The deposit was separated through filtration, and the solution was purified through reversed-phase middle-pressure liquid chromatography [ODS-AS-360-CC (by YMC), mobile phase: water-acetonitrile-0.1% trifluoroacetic acid]. The resulting fraction was diluted with ethyl acetate, washed with aqueous saturated sodium bicarbonate, and dried with anhydrous sodium sulfate. The solvent was evaporated away under reduced pressure to obtain the entitled compound as a brown solid.

1. customthe reaction liquid
2. customThe deposit was separated through filtration
3. customthe solution was purified through reversed-phase middle-pressure liquid chromatography [ODS-AS-360-CC (by YMC), mobile phase: water-acetonitrile-0.1% trifluoroacetic acid]
4. additionThe resulting fraction was diluted with ethyl acetate
5. washwashed with aqueous saturated sodium bicarbonate
6. dry with materialdried with anhydrous sodium sulfate
7. customThe solvent was evaporated away under reduced pressure