Potassium Iodide → HCID 58280257, compound

Participants

Reaction Steps

Add 147.5 mg (0.996 mmol) of 4-bromobutyronitrile at RT to a mixture of 200 mg (0.498 mmol) of (+/−)-5-(4-methoxyphenyl)-6-phenyl-4-(piperidin-3-yloxy)furo[2,3-d]pyrimidine, 0.25 ml (1.5 mmol) of diisopropylethylamine and 8.3 mg of potassium iodide in 2 ml of THF. The mixture is stirred under reflux for 10 h. After adding a further 0.25 ml (1.5 mmol) of diisopropylethylamine and 147.5 mg (0.996 mmol) of 4-bromobutyronitrile, continue to stir under reflux overnight. After cooling to RT, dilute with dichloromethane, wash with satd. sodium hydrogencarbonate solution, remove the organic phase, dry over sodium sulphate and concentrate under reduced pressure. After purifying the residue by means of preparative RP-HPLC (eluent: acetonitrile/water gradient) 189 mg of the target product are obtained (81.1% of theory).

Provenance & Evidence