反应详情

(R)-tert-butyl 2-(4-chloro-3-fluorophenyl)morpholine-4-carboxylate (990 mg) was dissolved in 2 mL of dichloromethane and TFA (2 mL) was added. The solution was stirred at room temperature for 2 h. Solvents were evaporated. The residue was extracted with dichloromethane and 1N NaOH solution. The organic layer was dried and concentrated. The residue was dried in vacuum to afford (R)-2-(4-chloro-3-fluorophenyl)morpholine an oil (669 mg). 1H NMR (400 MHz, CHLOROFORM-d) δ ppm 2.11 (br. s., 1H) 2.72 (dd, J=12.38, 10.36 Hz, 1H) 2.86-3.04 (m, 2H) 3.07 (dd, J=12.38, 2.53 Hz, 1H) 3.79 (td, J=11.37, 3.03 Hz, 1H) 4.05 (dd, J=11.49, 2.40 Hz, 1H) 4.48 (dd, J=10.36, 2.53 Hz, 1H) 7.02-7.13 (m, 1H) 7.15-7.23 (m, 1H) 7.33-7.42 (m, 1H).

1. customSolvents were evaporated
2. extractionThe residue was extracted with dichloromethane and 1N NaOH solution
3. customThe organic layer was dried
4. concentrationconcentrated
5. customThe residue was dried in vacuum