反应详情

4-Dimethylaminopyridine (51 mg, 0.42 mmol) and N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (80 mg, 0.42 mmol) were added to a suspension of 2,5-dichloro-4-(5-chloro-6-cyclopropylpyridin-3-yloxy)benzoic acid (Preparation 220, 100 mg, 0.28 mmol) in dichloromethane (3 mL). The reaction mixture was stirred at room temperature for 20 minutes. Methylsulfonamide (40 mg, 0.42 mmol) was added and the reaction mixture was stirred at room temperature for 18 hours before concentrating in vacuo. The crude compound was purified by reverse phase column chromatography eluting with acetonitrile:water (from 5:95 to 95:5) followed by preparative HPLC to afford the title compound (15.1 mg, 12%).

1. stirringthe reaction mixture was stirred at room temperature for 18 hours
2. concentrationbefore concentrating in vacuo
3. customThe crude compound was purified by reverse phase column chromatography
4. washeluting with acetonitrile