反应详情

A suspension of 4-hydroxy-1-(phenylmethyl)-3-piperidinecarboxamide (5.62 g, 23.9 mmol) in THF (65 mL) was treated dropwise with borane-methyl sulphide complex (2M solution in THF, 26.4 mL, 52.8 mmol). After stirring for 0.5 h at room temperature, the reaction mixture was heated at 80° C. for 1.5 h. Methanol (16 mL) was added and heating continued for 0.5 h. The mixture was evaporated and the residue was chromatographed on silica gel, eluting with 10-30% (2M ammonia/methanol)/dichloromethane to give the product (2.67 g, 51%).

1. temperaturethe reaction mixture was heated at 80° C. for 1.5 h
2. temperatureheating
3. waitcontinued for 0.5 h
4. customThe mixture was evaporated
5. customthe residue was chromatographed on silica gel
6. washeluting with 10-30% (2M ammonia/methanol)/dichloromethane