Potassium Carbonate → 3-(3,5-difluorophenyl)-5-[2-(morpholin-4-yl)ethoxy]-2-(pyridin-3-yl)-1H-inden-1-one

温度

80 °C

To a solution of 3-(3,5-difluorophenyl)-5-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one (60 mg, 0.18 mmol) obtained in Step 5 in DMF (2 mL) was added K2CO3(75 mg, 0.54 mmol) and 4-(2-chloroethyl)morpholine hydrochloride (50 mg, 0.27 mmol). The mixture was heated to 80° C. for 3 h and cooled to room temperature. The resulting solution was diluted with H2O and extracted with EtOAc (5 mL×3). The extracts were washed with H2O and brine, dried over MgSO4, and concentrated in vacuo. The residue was purified by silica gel column chromatography (2% MeOH/CH2Cl2) to afford the title compound (55 mg, 68%).

1. temperaturecooled to room temperature
2. extractionextracted with EtOAc (5 mL×3)
3. washThe extracts were washed with H2O and brine
4. dry with materialdried over MgSO4
5. concentrationconcentrated in vacuo
6. customThe residue was purified by silica gel column chromatography (2% MeOH/CH2Cl2)

ORDレコード

ord-2e197b0da2014b7396654b9bda743124

出典データセット

uspto-grants-2014_11

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08877747B2