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0 °C

42 g (0.50 mol) sodium acetate were added in portions to 73 g (0.25 mol) N-propylpiperazine dihydrobromide in 1 l methanol at 40° C. Subsequently, this was cooled to 0° C. and 50 g (0.25 mol) Boc-4-piperidon and 16 g (0.25 mol) sodium cyanoborohydride, in portions, were added, one after the other. Everything was then stirred at room temperature for 16 h. The reaction mixture was concentrated in a vacuum and then distributed between ethyl acetate and 1M NaOH. The organic phase was separated, washed with 1M NaOH, H2O and conc. NaCl solution, dried and concentrated in a vacuum. The residue was chromatographically purified over silica gel (mobile phase: MeOH/CH2Cl2=1/15). 43.6 g of the product were obtained.

1. concentrationThe reaction mixture was concentrated in a vacuum
2. customThe organic phase was separated
3. washwashed with 1M NaOH, H2O and conc. NaCl solution
4. customdried
5. concentrationconcentrated in a vacuum
6. customThe residue was chromatographically purified over silica gel (mobile phase: MeOH/CH2Cl2=1/15)