反应详情

To a solution containing 54.6 g of benzyl(R)-3-[chlorocarbonyl-(R)-1-(naphthalen-1-yl)ethylamino]piperidine-1-carboxylate dissolved in 700 ml of tetrahydrofuran was added 350 ml of water, and the mixture was stirred under reflux for 15 hours. After tetrahydrofuran was evaporated, a saturated aqueous sodium bicarbonate solution and chloroform were added thereto, the mixture was stirred and the liquids were separated. The organic layer was dried and concentrated, and the residue was purified by silica gel column chromatography (hexane:ethyl acetate=4:1→0:1) to obtain 24.3 g of benzyl(R)-3-[(R)-1-(naphthalen-1-yl)ethylamino]piperidine-1-carboxylate.

1. temperatureunder reflux for 15 hours
2. customAfter tetrahydrofuran was evaporated
3. additiona saturated aqueous sodium bicarbonate solution and chloroform were added
4. stirringthe mixture was stirred
5. customthe liquids were separated
6. customThe organic layer was dried
7. concentrationconcentrated
8. customthe residue was purified by silica gel column chromatography (hexane:ethyl acetate=4:1→0:1)