反应详情

温度

85 °C

To a mixture of ethyl 2-((R)-1-((S)-2-hydroxy-2-(4-((Z)—N′-hydroxycarbamimidoyl)phenyl)ethyl)piperidin-3-yl)acetate (18C-Isomer A) and sodium bicarbonate (378 mg, 4.50 mmol) in 2-propanol (10 mL) was added hydroxylamine hydrochloride (156 mg, 2.250 mmol). The reaction mixture was heated at 85° C. overnight. The reaction mixture was diluted with ethyl acetate and washed with H2O. The organic layer was dried with MgSO4, filtered, and concentrated to yield 346 mg of ethyl 2-((3R)-1-(2-hydroxy-2-(4-((Z)—N′-hydroxycarbamimidoyl)phenyl)ethyl)piperidin-3-yl)acetate. MS (M+1)=336. HPLC Peak RT=0.12 minutes.

1. washwashed with H2O
2. dry with materialThe organic layer was dried with MgSO4
3. filtrationfiltered
4. concentrationconcentrated