Diethyl 2-(piperidin-4-ylmethyl)malonate

Conditions: temp:62.51; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Benzyl chloride (54.4 g) and sodium carbonate (149.4 g) were added to the solution of the acetic acid salt of diethyl (4-piperidylmethyl)malonate [XXIXb] from the previous step. The obtained slurry was stirred for 12 hours at 60-65° C. and evaporated under reduced pressure. Water was added to the residue and the obtained mixture was extracted with dichloromethane. The organic layer was washed with water, dried over sodium sulfate, passed through short silica gel column and evaporated under reduced pressure. The obtained residue was washed with hexanes and dried under reduced pressure to give diethyl (N-benzyl-4-piperidylmethyl)malonate [XXIIb]. evaporated under reduced pressure Water was added to the residue the obtained mixture was extracted with dichloromethane The organic layer was washed with water dried over sodium sulfate evaporated under reduced pressure The obtained residue was washed with hexanes dried under reduced pressure