反应详情

(E)-3-[1-(3-Bromo-benzenesulfonyl)-1H-pyrrol-3-yl]-N-(tetrahydro-pyran-2-yloxy)-acrylamide (7.60 g) and 4-{2-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-ethyl}-morpholin (8.00 g) are dissolved in DME (300 mL). (Ph3P)3PdCl2 (2.40 g) and a 2M Na2CO3-solution (25 mL) are added and the mixture is heated 5 h to reflux temperature under an inert gas atmosphere. The reaction mixture is filtered and evaporated. After addition of a NaHCO3-solution and ethyl acetate, the organic phase is dried and evaporated. The crude product is purified by silica gel flash chromatography. 8.1 g of the title compound are obtained.

1. temperaturethe mixture is heated 5 h
2. temperatureto reflux temperature under an inert gas atmosphere
3. filtrationThe reaction mixture is filtered
4. customevaporated
5. additionAfter addition of a NaHCO3-solution and ethyl acetate
6. customthe organic phase is dried
7. customevaporated
8. customThe crude product is purified by silica gel flash chromatography