反应详情

温度

80 °C

To a mixture of 1-(1,1-dimethylethyl) 3-methyl 4-{[(trifluoromethyl)sulfonyl]oxy}-5,6-dihydro-1,3(2H)-pyridinedicarboxylate (2.5 g, P2), {4-[(trifluoromethyl)oxy]phenyl}boronic acid (1.52 g) and Pd(PPh3)4 (265 mg) under nitrogen, toluene (34 mL), ethanol (25 mL) and Na2CO3 (2M, 19 mL) were added in sequence. The mixture was stirred at 80° C. for 2 hours then the reaction mixture was allowed to reach room temperature. The aqueous phase was extracted with Et2O (2 times), the combined organic phases were dried on anhydrous Na2SO4 and the solvent was evaporated obtaining a crude product that was purified by flash-chromatography (eluting with ethyl acetate/cyclohexane from 1:9 to 3:7) to give the title compound (2.5 g)

1. customto reach room temperature
2. extractionThe aqueous phase was extracted with Et2O (2 times)
3. dry with materialthe combined organic phases were dried on anhydrous Na2SO4
4. customthe solvent was evaporated
5. customobtaining a crude product that
6. customwas purified by flash-chromatography (eluting with ethyl acetate/cyclohexane from 1:9 to 3:7)