反应详情

A mixture of 3-acetyl-4-trifluoromethylsulfonyloxy-6-methyl-1-ethoxycarbonylmethyl-2-pyridinone from step 2 above (2.5 g, 7.2 mmol), 2-isopropylbenzeneboronic acid (1.8 g, 11 mmol), potassium carbonate (1.5 g, 11 mmol), and Pd(PPh3)4 (1.7 g, 1.4 mmol) was heated to reflux under inert atmosphere for 3 h. The solvent was removed under reduced pressure and the residue was purified by flash column chromatography using a gradient elution of 25-75% EtOAc:hexanes to give the title compound (0.72 g; HPLC RT=21.79 min, method B).

1. temperaturewas heated
2. temperatureto reflux under inert atmosphere for 3 h
3. customThe solvent was removed under reduced pressure
4. customthe residue was purified by flash column chromatography
5. washa gradient elution of 25-75% EtOAc