Triethylamine → 4-[[2-(5-Bromo-2-fluorophenyl)pteridin-4-yl]amino]nicotinic Acid Methyl Ester

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-(5-bromo-2-fluorophenyl)-4-chloropteridine 106 (200 mg, 0.589 mmol), 4-aminonicotinic acid methyl ester (224 mg, 1.47 mmol) in dichloroethane (5 mL), was added dropwise triethylamine (300 μL, 2.07 mmol). The resulting mixture was heated at 70° C. for 15 min, then quenched with silica and purified by column chromatography (AcOEt/CH2Cl2/triethylamine, 70/19/1). Crystallization from AcOEt/Et2O afforded 200 mg of the title product 107 as yellow prisms (LCMS analysis).

Provenance & Evidence