反应详情

(S)-4-(2-(2-(4-carboxyphenylsulfonamido)acetoxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide (30 mg, 0.045 mmol), morpholine (19.76 mg, 0.227 mmol), DMAP (11.08 mg, 0.091 mmol) and EDC (43.5 mg, 0.227 mmol) were dissolved in DMF (1.5 ml). The reaction was stirred at RT overnight. The reaction mixture was diluted with water and extracted with EtOAc. The organic phase was dried over Na2SO4 and concentrated under vacuum. The crude product was purified by preparative reverse-phase HPLC to give (S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(2-(4-(morpholine-4-carbonyl)phenylsulfonamido)-acetoxy)ethyl)pyridine 1-oxide (15 mg, 0.021 mmol, 45.3% yield).

1. extractionextracted with EtOAc
2. dry with materialThe organic phase was dried over Na2SO4
3. concentrationconcentrated under vacuum
4. customThe crude product was purified by preparative reverse-phase HPLC