反应详情

温度

80 °C

A mixture of 1-(2-bromo-chlorobenzoyl)-2,3-dihydro-4-pyridinone (Preparation 3) (300 mg, 0.954 mmol), triethylamine (0.39 mmol, 0.54 ml), formic acid (0.05 ml, 1.3 mmol) and di(triphenylphosphine) diacetoxypalladium (47 mg, 0.063 mmol) in DMF (3 ml) was heated to 80° C. for 2 h. The cooled solution was filtered through celite, diluted with water, extracted twice with ethyl acetate, the extracts dried over sodium sulphate and evaporated. The residue was purified by flash column chromatography on silica eluting with 50% ethyl acetate in hexane to yield the title compound as a colourless oil (70 mg). MS (+CI) m/z 235/237 [M+H]+.

1. filtrationThe cooled solution was filtered through celite
2. additiondiluted with water
3. extractionextracted twice with ethyl acetate
4. dry with materialthe extracts dried over sodium sulphate
5. customevaporated
6. customThe residue was purified by flash column chromatography on silica eluting with 50% ethyl acetate in hexane