反应详情

To a solution of (±)-3,3-difluoro-4-(3-methoxy-4-nitro-phenyl)-piperidine-1-carboxylic acid tert-butyl ester (230.00 mg) in methanol (10 mL) was added palladium on carbon 10% (10:90, palladium:carbon black, 40 mg). The mixture was shaken in a Parr apparatus under an atmosphere of hydrogen (35 PSI) for 2 h. Filtration through Celite and evaporation of the solvent provided (±)-4-(4-amino-3-methoxy-phenyl)-3,3-difluoro-piperidine-1-carboxylic acid tert-butyl ester (200 mg, 95% yield), which was used without purification. 1H NMR (CDCl3): δ ppm 6.65-6.77 (m, 3H), 4.15-4.65 (m, 2H), 3.85 (s, 3H), 3.77 (br. s., 2H), 2.72-3.13 (m, 3H), 2.03-2.24 (m, 1H), 1.85 (d, J=12.4 Hz, 1H), 1.49 (s, 9H) 3124-67

1. filtrationFiltration
2. customthrough Celite and evaporation of the solvent