反应详情

5-[2-Fluoro-4-(methylsulfonyl)phenyl]-2-pyrazinamine (0.30 g, 50%) was prepared as a yellowish brown solid from 2-amino-5-bromopyrazine (0.4 g, 2.23 mmol), [2-fluoro-4-(methylsulfonyl)phenyl]boronic acid (0.50 g, 2.23 mmol), 2M Na2CO3 (4 mL), Pd(PPh3)4 (52 mg, 0.05 mmol) in 1,4-dioxane (8 mL) and MeOH (4 mL) in a manner similar to Example 145, Step 1. The crude product was triturated with CH2Cl2 to give 5-[2-fluoro-4-(methylsulfonyl)phenyl]-2-pyrazinamine as a yellowish brown solid. 1H NMR (400 MHz, DMSO-d6): δ 8.41 (s, 1H), 8.11 (t, 1H, J=8.0 Hz), 8.01 (s, 1H), 7.85-7.75 (m, 2H), 6.91 (s, 2H), 3.26 (s, 3H); LRMS (ESI), m/z 268 (M+H).

1. customThe crude product was triturated with CH2Cl2