反应详情

Prepared from (4-(7-(4-amino-2-fluorophenoxy)thieno[3,2-b]pyridin-2-yl)phenyl)(morpholino)methanone (Example 129, Step A) and 4-(4-fluorophenyl)-3-oxo-3,4-dihydropyrazine-2-carboxylic acid according to the procedure of Example 89. The crude was purified by silica gel flash column chromatography (3 to 5% MeOH in CH2Cl2) to afford 47 mg (72%) of the desired product. LRMS (APCI pos) m/e 666.2 (M+1). 1H-NMR (400 MHz, CDCl3/CD3OD) δ 8.47 (d, 1H), 8.06 (dd, 1H), 7.93 (d, 2H), 7.90 (d, 1H), 7.87 (s, 1H), 7.82 (d, 1H), 7.59 (m, 4H), 7.52 (d, 1H), 7.40 (t, 1H), 7.34 (m, 3H), 6.67 (d, 1H), 3.69-3.79 (m, 8H); 19F NMR (376 MHz, CDCl3/CD3OD) δ −112.7, −128.7.

1. customThe crude was purified by silica gel flash column chromatography (3 to 5% MeOH in CH2Cl2)