反应详情

温度

80 °C

A mixture of Example 36D (0.800 g, 1.380 mmol), 6-bromo-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-benzo[d][1,2,3]triazole (0.450 g, 1.519 mmol), PdCl2(dppf)-CH2Cl2 adduct (0.045 g, 0.055 mmol), and aqueous sodium bicarbonate (6 mL, 1.380 mmol) in N,N-dimethylformamide (20 mL) was degassed and the mixture was heated at 80° C. for 2.5 hours. The reaction mixture was diluted with ethyl acetate and washed with aqueous NaHCO3/brine and water, dried over MgSO4, filtered, and purified on a 40 g column using the ISCO Companion flash system eluting with heptanes/ethyl acetate (4:6 to 3:7) to give the title compound.

1. washwashed with aqueous NaHCO3/brine and water
2. dry with materialdried over MgSO4
3. filtrationfiltered
4. custompurified on a 40 g column
5. washeluting with heptanes/ethyl acetate (4:6 to 3:7)