Sodium Carbonate → 6-{[6-(2-Methoxyphenyl)-5-(4-methoxyphenyl)furo[2,3-d]pyrimidin-4-yl]amino}hexanoic acid methyl ester

Participants

Reaction Conditions

Reaction Steps

Add 0.45 ml of a 2 M aqueous sodium carbonate solution to a mixture of 200 mg (0.45 mmol) 6-{[6-bromo-5-(4-methoxyphenyl)furo[2,3-d]pyrimidin-4-yl]amino}hexanoic acid methyl ester and 16 mg (0.02 mmol) bis(triphenylphosphine)palladium(II) chloride in 10 ml dimethylsulphoxide. Next, add 85 mg (0.56 mmol) (2-methoxyphenyl)boronic acid and stir the mixture for 15 h at 80° C. Filter the reaction mixture and purify directly by preparative RP-HPLC (gradient: water/acetonitrile). 63 mg (42% of theor.) of the desired product is obtained.

Provenance & Evidence