Potassium Phosphate, Tribasic → (S)-methyl 2-(4-fluorophenyl)-7-methoxy-3-(2-methylpyrrolidin-1-yl)quinoxaline-6-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a solution of (S)-methyl 7-methoxy-3-(2-methylpyrrolidin-1-yl)-2-(trifluoromethylsulfonyloxy)quinoxaline-6-carboxylate (300 mg, crude) in dioxane (5 ml) and water (3 drops) was added (4-fluorophenyl)boronic acid (280.6 mg, 2.01 mmol), Pd(PPh3)4 (38.5 mg, 0.03 mmol), and K3PO4 (422 mg, 1.99 mmol), and the reaction was stirred for 40 minutes at 95° C. under an atmosphere of nitrogen. The reaction mixture was concentrated in vacuo to give a residue, which was purified via silica gel column chromatography (1% ethyl acetate in petroleum ether) to afford (S)-methyl 2-(4-fluorophenyl)-7-methoxy-3-(2-methylpyrrolidin-1-yl)quinoxaline-6-carboxylate as a light yellow solid (200 mg).

Provenance & Evidence