反应详情

A mixture of 2-(hydroxymethyl)phenylboronic acid (1 g, 7 mmol), 5-(4-bromo-2-fluorophenyl)pyrazin-2-amine (1.76 g, 6.6 mmol), Pd(dppf)Cl2.CH2Cl2 (483 mg, 0.66 mmol) and Na2CO3 (2.1 g, 20 mmol) in DMF (50 mL) was stirred at 110° Celsius overnight under N2. The solution was concentrated to dryness and the residue purified by FCC to give (4′-(5-aminopyrazin-2-yl)-5′-fluorobiphenyl-2-yl)methanol (1.2 g, 62%). 1H NMR (300 MHz, DMSO-d6) δ 8.38 (s, 1H), 8.02 (d, J=1.4, 1H), 7.90 (m, 1H), 7.57 (d, J=7.4, 1H), 7.49-7.26 (m, 5H), 6.69 (s, 2H), 5.20 (t, J=5.3, 1H), 4.44 (d, J=5.3, 2H).

1. concentrationThe solution was concentrated to dryness
2. customthe residue purified by FCC