反应详情

Using the method of Example 32, 3-(2-(4-methylthiazol-2-ylamino)pyridin-4-yloxy)benzoic acid (0.1 g, 0.3055 mmol), triethylamine (0.2129 mL, 1.527 mmol), ethyl carbonochloridate (0.03359 mL, 0.3513 mmol), and 3-morpholinopropan-1-amine (0.1339 mL, 0.9164 mmol) were reacted in THF (2 mL) to provide 3-(2-(4-methylthiazol-2-ylamino)pyridin-4-yloxy)-N-(3-morpholinopropyl)benzamide dihydrochloride (0.098 g, 60.33% yield) as off white solid. 1H NMR (CDCl3) δ 8.52 (s, 1H), 8.19 (d, 1H), 7.91 (d, 1H), 7.74 (s, 1H), 7.54 (t, 1H), 7.24 (d, 1H), 6.82 (dd, 1H), 6.41 (s, 1H), 4.26 (m, 2H), 3.99 (m, 2H), 3.65 (m, 2H), 3.52 (m, 2H), 3.19 (t, 2H), 2.89 (m, 2H), 2.41 (d, 3H), 2.26 (m, 2H); Mass spectrum (esi) m/z=454 (100) (M+H).