反应详情

In methanol (10 ml) were dissolved 2-amino-5-chloro-α-(3-tert-butoxycarbonylaminomethylphenyl)benzyl alcohol produced in Example (1) (0.5 g) and 4-fluorobenzaldehyde (0.2 g). To the solution were added acetic acid (0.1 g) and cyano sodium borohydride (0.1 g). The mixture was concentrated, to which were added water (60 ml) and ethyl acetate (50 ml), followed by extraction. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was then distilled off to leave 5-chloro-2-(4-fluorobenzylamino)-α-(3-tert-butoxycarbonylaminomethylphenyl)benzyl alcohol (0.56 g) as a colorless oily product.

1. concentrationThe mixture was concentrated, to which
2. additionwere added water (60 ml) and ethyl acetate (50 ml)
3. extractionfollowed by extraction
4. washThe organic layer was washed with water
5. dry with materialdried over anhydrous sodium sulfate
6. distillationThe solvent was then distilled off