Potassium Carbonate → HCID 66612102, compound

Participants

Reaction Steps

2,2,2-Trifluoro-1-(5-iodo-7-nitro-3,4-dihydro-1H-isoquinolin-2-yl)ethanone (0.8 g, 2 mmoles) and 2-chlorophenyl boronic acid (0.31 g, 2 mmoles) were stirred with an acetonitrile water mixture (50:50, 28 mls). Anhydrous potassium carbonate (0.55 g, 4 mmoles) was then added under a stream of nitrogen. To this solution was then added palladium tetra(triphenyl phosphine) (tetrakis, 0.12 g, catalytic) and the solution heated (95° C.) for three hours. The reaction mixture was cooled to room temperature and water (10 mls) added followed by dichloromethane (3×60 mls), the combined dichloromethane extracts were washed with brine (20 mls) and dried over magnesium sulphate. The solution was then filtered and evaporated to leave an orange gum which was then dissolved in ether (20 mls) to which was added HCl/MeOH (4M) dropwise to afford a beige precipitate which was collected and dried (0.62 g, 95%, 90% pure).

Provenance & Evidence