反应详情

温度

100 °C

Tert-butyl N-[5-bromo-3-(5-phenyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl]-N-tert-butoxycarbonyl-carbamate (2.4633 g, 4.752 mmol) was dissolved in DMF (19.24 mL) and tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-2H-pyridine-1-carboxylate (2.204 g, 7.128 mmol) and Pd(PPh3)2Cl2 (196.6 mg, 0.4752 mmol) were added followed by Na2CO3 (7.130 mL of 2 M, 14.26 mmol) and the reaction heated at 100° C. under nitrogen for 15 minutes. The reaction mixture was allowed to cool to RT and the solvent removed in vacuo. The mixture was diluted with EtOAc/water and the organic layer washed with water (×4) followed by brine (×3). After drying over MgSO4, the reaction was filtered and evaporated to dryness to give a dark brown oil which was purified on silica gel by flash column chromatography (0-40% EtOAc/Petrol) to afford the title compound (2.40 g, 81% Yield).

1. temperatureto cool to RT
2. customthe solvent removed in vacuo
3. additionThe mixture was diluted with EtOAc/water
4. washthe organic layer washed with water (×4)
5. dry with materialAfter drying over MgSO4
6. filtrationthe reaction was filtered
7. customevaporated to dryness
8. customto give a dark brown oil which
9. customwas purified on silica gel by flash column chromatography (0-40% EtOAc/Petrol)