2-(4-(2-Aminopyridin-4-yloxy)-3-fluorophenylamino)-n-(2,4-difluorophenyl)nicotinamide, hydrochloride salt → 4-(4-(2-Aminopyridin-4-yloxy)-3-fluorophenylamino)-n-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamide, trihydrochloride salt

Participants

Reaction Steps

4-(4-(2-Carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamide (55 mg, 0.01 mmol) was converted to the title compound (16 mg, 26%) in a manner similar to the preparation of 2-(4-(2-aminopyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)nicotinamide (Step E of Example 3). 1H NMR (DMSO-d6) δ 11.24 (s, 1H), 10.20 (s, 1H), 8.85 (s, 1H), 7.92 (m, 2H), 7.82 (br s, 2H), 7.48-7.35 (m, 4H), 7.08 (m, 1H), 6.65 (dd, 1H, J=7.3, 2.5 Hz), 6.12 (d, 1H, J=2.4 Hz), 3.74 (m, 4H) 3.63 (m, 4H); MS(ESI+) m/z 538 (M+H)+.

Provenance & Evidence