Sodium Carbonate → 4-{[(3R)-1-Benzylpiperidin-3-yl]oxy}-5-(4-ethylphenyl)-6-(2-fluorophenyl)furo[2,3-d]pyrimidine

Participants

Reaction Conditions

Reaction Steps

Add 0.68 ml of a 2 M aqueous sodium carbonate solution to a mixture of 365 mg (0.68 mmol) of 4-{[(3R)-1-benzylpiperidin-3-yl]oxy}-5-(4-ethylphenyl)-6-iodofuro[2,3-d]pyrimidine and 24 mg (0.03 mmol) of bis(triphenylphosphine)palladium(II) chloride in 15 ml of DMSO. Then add 118 mg (0.85 mmol) of (2-fluorophenyl)boronic acid and stir the mixture at 80° C. for 15 hours. Then filter the reaction mixture and purify directly by means of preparative RP-HPLC (gradient: water/acetonitrile). 291 mg (84% of theory) of the target compound are obtained.

Provenance & Evidence