反应详情

温度

80 °C

Dissolve 4-benzyl-2-(2-chloro-4-fluoro-phenyl)morpholine (529 mg, 1.73 mmol) in DCM (2.5 mL). Add 1-chloroethyl chloroformate (1.25 g, 8.65 mmol); heat to 80° C.; and stir overnight. Add MeOH (2.5 mL) and stir at 65° C. for 3 hours. Concentrate under reduced pressure and purify via SCX chromatography eluting with a gradient of 0-100% of (2N NH3/MeOH) in MeOH. Combine the product fractions and remove the solvents under reduced pressure to provide the title compound as a white solid (345 mg, 92%). MS (m/z): 216 (M+1).

1. concentrationConcentrate under reduced pressure
2. custompurify via SCX chromatography
3. washeluting with a gradient of 0-100% of (2N NH3/MeOH) in MeOH
4. customremove the solvents under reduced pressure