反应详情

To a solution of (S)-2-(1-{[2-chloro-4-(4-fluorophenyl)quinolin-7-yl]methyl}-1H-1,2,3-triazol-4-yl)-1,1,1-trifluorobutan-2-ol (100 mg, 0.22 mmol) in DME (5 mL) was added Pd(PPh3)4 (12 mg, 0.01 mmol), phenylboronic acid (34 mg, 0.29 mmol) and sodium carbonate (2M, 0.2 mL, 0.44 mmol). The mixture was refluxed for 14 h. The reaction was quenched with saturated aqueous NH4Cl and extracted with EtOAc. The combined organic layers were washed with brine, dried over Na2SO4, filtered and concentrated under reduced pressure. Purification on silica gel (eluting with acetone/dichloromethane, 1:9) gave the title compound. MS (+ESI): 507. (M+H)+.

1. temperatureThe mixture was refluxed for 14 h
2. customThe reaction was quenched with saturated aqueous NH4Cl
3. extractionextracted with EtOAc
4. washThe combined organic layers were washed with brine
5. dry with materialdried over Na2SO4
6. filtrationfiltered
7. concentrationconcentrated under reduced pressure
8. customPurification on silica gel (eluting with acetone/dichloromethane, 1:9)