反应详情

To a solution of tert-butyl 4-{4-[4-(1-methyl-6-oxo-1,6-dihydro-[4,4′]bipyrimidinyl-2-yloxy)piperidin-1-yl]benzyl}piperazine-1-carboxylate (470 mg, 0.83 mmol) in dichloromethane (4.2 ml) was added trifluoroacetic acid (3.9 g, 34 mmol) at room temperature. The mixture was stirred overnight. After concentration under reduced pressure, the residue was dissolved into water. The aqueous solution was washed with ethyl acetate and basified with potassium carbonate. Extraction with chloroform was performed three times and the organic layer was dried over sodium sulfate, concentrated in vacuo to afford 1-methyl-2-[1-(4-piperazin-1-ylmethyl-phenyl)piperidin-4-yloxy]-1H-[4,4′]bipyrimidinyl-6-one as a pale yellow solid (260 mg, 0.56 mmol, 67%).

1. concentrationAfter concentration under reduced pressure
2. dissolutionthe residue was dissolved into water
3. washThe aqueous solution was washed with ethyl acetate
4. extractionExtraction with chloroform
5. dry with materialthe organic layer was dried over sodium sulfate
6. concentrationconcentrated in vacuo