Potassium Carbonate → (3R,4S)-N-benzyl-3-fluoro-1-(3-methoxy-4-nitrophenyl)piperidin-4-amine

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

DMA (60 ml) and potassium carbonate (5.65 g, 40.86 mmol) were added to the flask containing 4-fluoro-2-methoxy-1-nitrobenzene (1.748 g, 10.22 mmol) and (3R,4S)—N-benzyl-3-fluoropiperidin-4-amine HCl salt (INTERMEDIATE 46, 2.5 g, 10.22 mmol). The reaction was heated to 120° C. for 5 h. The reaction mixture was cooled to rt, and filtered. The filtrate was diluted with EtOAc (50 ml) and the solution was washed with brine (2×100 ml). The organic layer was dried over Na2SO4, filtered, and concentrated to give a crude yellow liquid. It was purified using silica gel chromatography (80-100% EtOAc/hexane) to give the title product (2.200 g, 59.9%). m/z 361.

Herkunft & Nachweise