Methanesulfonamide → HCID 58042470, compound

Participants

Reaction Steps

To a solution of 4-(5-chloro-6-(1,1,1,3,3,3-hexafluoropropan-2-yloxy)pyridin-3-ylamino)benzoic acid (Preparation 259, 116 mg, 0.27 mmol) in dichloromethane (5 mL) was added 4-dimethylaminopyridine (50 mg, 0.41 mmol) and N-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride (77 mg, 0.41 mmol). The solution was stirred for 25 minutes at room temperature and methanesulfonamide (39 mg, 0.41 mmol) was added. The reaction mixture was stirred for 18 hours at room temperature. The solution was concentrated in vacuo and the material was purified by reverse phase chromatography eluting with acetonitrile:water (from 5:95 to 95:5, 30 minutes gradient followed by 5 minutes isocratic) to afford the title compound as a white solid (98 mg, 74%).

Provenance & Evidence