反应详情

To a stirred solution of (1S,2R)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-phenylpropan-2-amine (18 mg, 50 μmol) in dichloromethane (2 ml) was added triethylamine (100 μl), followed by 2-chloro-1,1-dimethyl-2-oxoethyl acetate (24 mg, 150 μmol). The stirring was continued for 20 min at r.t., then the solvent was removed under reduced pressure, and the residue dissolved in ethanol (1 ml). Aqueous sodium hydroxide solution (1 M, 1 ml) was added, and the mixture was stirrer at 80° C. for 30 min. Then it was cooled to r.t., acidified with TFA, and concentrated under reduced pressure. The product was purified by semi-prep. HPLC. Yield 22 mg (96%).

1. customthe solvent was removed under reduced pressure
2. dissolutionthe residue dissolved in ethanol (1 ml)
3. additionAqueous sodium hydroxide solution (1 M, 1 ml) was added
4. customat 80° C.
5. customfor 30 min
6. concentrationconcentrated under reduced pressure
7. customThe product was purified by semi-prep