反应详情

温度

80 °C

A solution of 5.18 g (30 mmol) methyl 5-chloropyrazine-2-carboxylate in 150 ml degassed DMF was treated with 3.47 g (0.1 mmol) tetrakis(triphenylphosphine)palladium and heated at 80° C. 6.27 g (33 mmol) of 4-(trifluoromethyl)benzeneboronic acid and 14 66 g (45 mmol) of cesium carbonate were added and heated for 3.5 h. The reaction was cooled to RT and extracted with H2O (0° C.)/Et2O (3×). The organic phases were washed with aqueous 10% NaCl, dried (NaSO4) and evaporated. Purification by flash-chromatography on silica gel (heptane/AcOEt 95:5 to 2:1) gave 2.3 g (27%) of 5-(4-trifluoromethyl-phenyl)-pyrazine-2-carboxylic acid methyl ester.

1. temperatureheated for 3.5 h
2. temperatureThe reaction was cooled to RT
3. extractionextracted with H2O (0° C.)/Et2O (3×)
4. washThe organic phases were washed with aqueous 10% NaCl
5. dry with materialdried (NaSO4)
6. customevaporated
7. customPurification by flash-chromatography on silica gel (heptane/AcOEt 95:5 to 2:1)