反应详情

Add 0.5 ml of 2 M aqueous potassium carbonate solution to a mixture of 224 mg (0.50 mmol) 6-{[6-bromo-5-(4-methoxyphenyl)furo[2,3-d]pyrimidin-4-yl]amino}hexanoic acid methyl ester and 29 mg (0.03 mmol) tetrakis(triphenylphosphine)palladium(0) in 2.5 ml 1,2-dimethoxyethane. Next, add 119 mg (0.63 mmol) (2-trifluoromethyl)phenylboronic acid and stir the mixture for 15 h under reflux. Filter the reaction mixture and purify directly by preparative RP-HPLC (gradient: water/acetonitrile). 118 mg (46% of theor.) of the desired product is obtained.

1. temperatureunder reflux
2. filtrationFilter the reaction mixture
3. custompurify directly by preparative RP-HPLC (gradient: water/acetonitrile)