反应详情

温度

80 °C

To a mixture of 1-(2-{(3,5-bis-trifluoromethyl-benzyl)-[(3S,5R)-1-(2,5-dichloro-pyrimidin-4-yl)-5-ethyl-pyrrolidin-3-yl]-amino}-pyrimidin-5-yl)-3-methyl-imidazolidin-2-one (30 mg, 0.05 mmol) in i-PrOH (1 mL) is added piperidin-4-ol (23 mg, 0.23 mmol). The reaction mixture is stirred at 80° C. for 12 hours. After removal of solvent, the mixture is washed with brine and extracted with EtOAc. The combined organic layer is dried over MgSO4 then concentrated under reduced pressure to give 1-[2-((3,5-bis-trifluoromethyl-benzyl)-{(3S,5R)-1-[5-chloro-2-(4-hydroxy-piperidin-1-yl)-pyrimidin-4-yl]-5-ethyl-pyrrolidin-3-yl}-amino)-pyrimidin-5-yl]-3-methyl-imidazolidin-2-one (26 mg, 79%) after purification by silica gel column chromatography (eluent: EtOAc:MeOH=20:1).

1. customAfter removal of solvent
2. washthe mixture is washed with brine
3. extractionextracted with EtOAc
4. dry with materialThe combined organic layer is dried over MgSO4
5. concentrationthen concentrated under reduced pressure