[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]#[C:9][C:10]2[CH:11]=[N:12][CH:13]=[C:14]([O:16][CH3:17])[CH:15]=2)=[CH:4][C:3]=1[NH2:18].[C:19](OC(=O)C)(=[O:21])[CH3:20]>N1C=CC=CC=1>[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]#[C:9][C:10]2[CH:11]=[N:12][CH:13]=[C:14]([O:16][CH3:17])[CH:15]=2)=[CH:4][C:3]=1[NH:18][C:19](=[O:21])[CH3:20]Dissolve 2-fluoro-5-(5-methoxypyridin-3-ylethynyl)-phenylamine, (prepared as described in EXAMPLE 111), (200 mg, 0.83 mmol) in pyridine (3 mL) and add acetic anhydride (84 mg, 0.83 mmol). Stir under nitrogen at room temperature for 48 h and concentrate. Purify by silica gel chromatography, eluting with 100% ethyl acetate to give the title compound as a light yellow solid (180 mg, 76%).
Wird geladen…