反应详情

To a mixture of 2-[4-(1-methyl-6-oxo-1,6-dihydro-[4,4′]bipyrimidinyl-2-yloxy)piperidin-1-yl]benzaldehyde (80 mg, 0.20 mmol), morpholine (27 mg 0.31 mmol) and acetic acid (one drop) in 1,2-dichloroethane (1.0 ml) was added sodium triacetoxyborohydride (110 mg, 0.52 mmol). The mixture was stirred at room temperature for 2 hours. The mixture was partitioned between water and chloroform. The organic layer was washed with saturated aqueous sodium hydrogen carbonate, dried over sodium sulfate, and concentrated in vacuo. The residue was purified by silica gel column chromatography (eluent; chloroform/methanol=95/5) to afford 1-methyl-2-[1-(2-morpholin-4-ylmethyl-phenyl)piperidin-4-yloxy]-1H-[4,4′]bipyrimidinyl-6-one as a colorless solid (63 mg, 0.14 mmol, 67%).

1. customThe mixture was partitioned between water and chloroform
2. washThe organic layer was washed with saturated aqueous sodium hydrogen carbonate
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated in vacuo
5. customThe residue was purified by silica gel column chromatography (eluent; chloroform/methanol=95/5)