反应详情

温度

110 °C

To 4-(3-chloro-1-propyn-1-yl)-2-(methyloxy)-1-nitrobenzene (Example 139, step B) (0.250 g, 1.1 mmol) in 10 mL of dioxane was added, 1-methylpiperazine (0.31 g, 3.1 mmol). The mixture was heated to 110° C. for 3 h. The mixture was purified by flash chromatography to give the title compound of step A (0.309 g, 1.07 mmol, 97%). 1H NMR (400 MHz, CDCl3) δ ppm 7.78 (d, J=8.24 Hz, 1H), 7.11 (s, 1H), 7.04 (dd, J=8.33, 1.56 Hz, 1H), 3.94 (s, 3H), 3.55 (s, 2H), 2.64-2.78 (m, 4H), 2.47-2.62 (m, 4H), 2.33 (s, 3H).

1. customThe mixture was purified by flash chromatography