反应详情

7-Bromoisoquinolin-3-amine (15.0 g, 67.4 mmol), 5-fluoro-2-methylphenylboronic acid (12.4 g, 81.0 mmol), Pd(dppf)Cl2 (2.76 g, 3.38 mmol) and Cs2CO3 (26.4 g, 81.0 mmol) in MeCN/H2O (10:1, 150 mL) was stirred at 120° C. for 6 h under N2. After the reaction mixture was filtered, the filtrate was concentrated and purified by chromatography on silica gel to give the desired product (13.5 g, 79.4%). LCMS (ESI): RT (min)=0.869, M+H+=252.8, method=A. 1H NMR (400 MHz, DMSO-d6) δ 8.84 (s, 1H), 7.75 (s, 1H), 7.55 (d, J=8.8 Hz, 1H), 7.44 (d, J=8.4 Hz, 1H), 7.34-7.30 (m, 1H), 7.11-7.07 (m, 2H), 6.64 (s, 1H), 6.00 (s, 2H), 2.22 (s, 3H).

1. filtrationAfter the reaction mixture was filtered
2. concentrationthe filtrate was concentrated
3. custompurified by chromatography on silica gel