反应详情

6.1 g of methyl 1-benzylpiperidine-4-carboximidate dihydrochloride was distributed into an aqueous solution of potassium carbonate and ethyl acetate under ice-cooling. The organic layer was extracted and dried over anhydrous sodium sulfate. After distilling off the solvent under reduced pressure, 4.7 g of free methyl 1-benzylpiperidine-4-carboximidate was obtained as a colorless oily substance. A solution of 2.35 g of methyl 1-benzylpiperidine-4-carboximidate and 0.95 g (10 mmol) of methanesulfonamide in dry methanol was stirred at room temperature for 3 days. Subsequently, 1.0 g of palladium-carbon was added to the reaction mixture and the resulting mixture was stirred in a hydrogen atmosphere under atmospheric pressure for 1 hour. The inorganic matters were eliminated by filtering through celite. After distilling off the solvent under reduced pressure, the residue was recrystallized from methanol to thereby give 1.38 g of the title compound as colorless needles.

1. temperaturecooling
2. extractionThe organic layer was extracted
3. dry with materialdried over anhydrous sodium sulfate
4. distillationAfter distilling off the solvent under reduced pressure