反应详情

1.26 g (20.0 mmol) NaBH3CN were added in 4 batches at RT to a solution of 1.71 g (5.0 mmol) tert. butyl 4-piperazin-1-yl-piperidine-1-carboxylate and 0.75 mL (10.0 mmol) cyclopropanecarbaldehyde in 100 mL of EtOH and the reaction mixture was stirred overnight at RT. The mixture was evaporated down i.vac., the residue was taken up in saturated NaHCO3 solution, extracted exhaustively with EtOAc and the organic phase was dried over Na2SO4. After the desiccant and solvent had been eliminated the residue was purified by chromatography (silica gel, EtOAc/MeOH/NH3 90:10:0.5).

1. customThe mixture was evaporated down i.vac
2. extractionextracted exhaustively with EtOAc
3. dry with materialthe organic phase was dried over Na2SO4
4. customwas purified by chromatography (silica gel, EtOAc/MeOH/NH3 90:10:0.5)