反应详情

温度

120 °C

2-(2-Fluoro-4-methoxy-phenyl)-2-hydroxy-propylamine hydrochloride was converted to the free base by partitioning between ethyl acetate and 1 M NaOH. The amine (1.0 g, 5.02 mmol) was combined with propane-2-sulfonic acid benzotriazol-1-yl ester (1.3 g, 5.52 mmol) in DMF (25 mL) and heated at 120° C. for 2 hr. then cooled to room temperature. The reaction mixture was diluted with ethyl acetate and extracted with 1 M HCl. The organic layer was separated and washed with water and saturated NaCl, dried (MgSO4), filtered, and concentrated to a yellow oil which was used in the next step without purification.

1. customby partitioning between ethyl acetate and 1 M NaOH
2. temperaturethen cooled to room temperature
3. extractionextracted with 1 M HCl
4. customThe organic layer was separated
5. washwashed with water and saturated NaCl
6. dry with materialdried (MgSO4)
7. filtrationfiltered
8. concentrationconcentrated to a yellow oil which
9. customwas used in the next step without purification