反应详情

Piperidine a14 (0.7 g, 8.3 mmol, 1.5 eq) is added to a suspension of [(2S)-5-oxopyrrolidin-2-yl]methyl 4-methylbenzenesulfonate a13 (1.5 g, 5.56 mmol, 1 eq) and potassium carbonate (1.5 g, 11.1 mmol, 2 eq) in acetonitrile (50 ml), and the mixture is stirred at reflux overnight. Potassium carbonate is filtered and the solvent is removed in vacuo. The residue is dissolved in a minimum of dichloromethane, then the organic layer is sonicated and heated to precipitate a white solid which is filtered. The liquid phase is concentrated in vacuo to give 1 g of (5S)-5-(piperidin-1-ylmethyl)pyrrolidin-2-one a15 as a yellow oil.

1. temperatureat reflux overnight
2. filtrationPotassium carbonate is filtered
3. customthe solvent is removed in vacuo
4. dissolutionThe residue is dissolved in a minimum of dichloromethane
5. customthe organic layer is sonicated
6. temperatureheated
7. customto precipitate a white solid which
8. filtrationis filtered
9. concentrationThe liquid phase is concentrated in vacuo