Hydrochloric Acid → HCID 71293599, compound

Participants

Reaction Steps

To a stirred solution of 4-{[(5-{4-[4-({[(2-fluoro-5-methylphenyl)amino]carbonyl}amino)phenoxy]pyridin-2-yl}-1H-pyrrol-3-yl)carbonyl]amino}butanoic acid (300 mg, 0.56 mmol) in 10 ml of anhydrous DMF were added HATU (255 mg, 0.67 mmol) and N,N-diisopropylethylamine (217 mg, 1.68 mmol). The mixture was stirred at room temperature for 10 minutes, followed by addition of 2-methoxyethanol (0.50 ml, 6.3 mmol). The mixture was heated at 66° C. for 1 hour, and poured into 100 ml of water with vigorous stirring. 1M HCl was added dropwise until pH=4. The precipitates were filtered, washed with water and dried in vacuo to give the crude, which was purified by silica gel chromatography eluting with ethyl acetate to give 2-methoxyethyl 4-{[(5-{4-[4-({[(2-fluoro-5-methylphenyl)amino]carbonyl}amino)phenoxy]pyridin-2-yl}-1H-pyrrol-3-yl)carbonyl]amino}butanoate as white solid. Yield: 215 mg, 65%.

Provenance & Evidence