反应详情

Prepared from (4-(7-(4-amino-2-fluorophenoxy)thieno[3,2-b]pyridin-2-yl)phenyl)(morpholino)methanone (prepared as in Example 129, Step A) and 4-methyl-3-oxo-3,4-dihydropyrazine-2-carboxylic acid (prepared from methyl 3-oxo-3,4-dihydropyrazine-2-carboxylate with iodomethane and followed by hydrolysis using the methods described in Example 149, Steps A and B) according to the procedure of Example 89. The crude was purified by silica gel flash column chromatography (5% MeOH in CH2Cl2) to afford 6.6 mg (25%) of the desired product. LRMS (APCI pos) m/e 586.2 (M+1). 1H-NMR (400 MHz, CDCl3/CD3OD) δ 8.47 (d, 1H), 8.07 (dd, 1H), 7.92 (m, 3H), 7.86 (s, 1H), 7.76 (d, 1H), 7.55 (m, 3H), 7.39 (t, 1H), 6.67 (d, 1H), 3.75 (s, 3H), 3.55-3.80 (m, 8H); 19F NMR (376 MHz, CDCl3/CD3OD) δ −128.3.

1. customfollowed by hydrolysis
2. customThe crude was purified by silica gel flash column chromatography (5% MeOH in CH2Cl2)