Potassium Phosphate, Tribasic → HCID 89444312, compound

Participants

Reaction Conditions

Reaction Steps

In a sealed tube were added methyl 4-[(5-bromopyrazin-2-yl)amino]-4-oxo-butanoate (A2, 1.00 g, 3.47 mmol), K3PO4 (2.58 g), palladium (II) acetate (0.0795 g), tricyclohexyl phosphine (0.195 g), cyclopropylboronic acid (0.447 g), toluene (3 mL) and water (0.05 mL). Argon was bubbling through the mixture for ca. 5 min. The mixture was then heated under microwave irradiation for 5 min at 150° C. The mixture was diluted with ethyl acetate, washed with water and brine, dried and evaporated. The product was purified by flash chromatography (AcOEt/cyclohexane: 1/99→99/1) to give methyl 4-[(5-cyclopropylpyrazin-2-yl)amino]-4-oxo-butanoate (A31, 0.020 g, 0.080 mmol, 2.31% Yield). 1H NMR (400 MHz, CDCl3) 9.28 (1H, s), 8.24 (1H, s), 8.10 (1H, s), 3.72 (3H, s), 2.75-2.65 (4H, m), 2.00 (1H, m), 1.00 (4H, m).

Provenance & Evidence