反应详情

A solution of ((R)-1-benzyl-2-oxo-ethyl)-carbamic acid tert-butyl ester (0.5 g, 2.0 mmol), (4-fluoro-phenyl)-piperidin-4-yl-methanone (0.414 g, 2.0 mmol) and sodium triacetoxyborohydride (0.638 g, 3.0 mmol) in tetrahydroftiran (20 ml) is stirred at ambient temperature for 24 hours. The solvent is evaporated and the residue redissolved in dichloromethane and washed with saturated sodium bicarbonate solution. The dichloromethane is dried over magnesium sulphate and evaporated. The crude product is purified by flash silica chromatography (ethylacetate:hexane, 3:1 elution) to afford {(R)-1-benzyl-2-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-ethyl}carbamic acid tert-butyl ester. [MH]+441.3.

1. customThe solvent is evaporated
2. dissolutionthe residue redissolved in dichloromethane
3. washwashed with saturated sodium bicarbonate solution
4. dry with materialThe dichloromethane is dried over magnesium sulphate
5. customevaporated
6. customThe crude product is purified by flash silica chromatography (ethylacetate:hexane, 3:1 elution)