Ethyl 4-(2-aminoethyl)-1-benzyl-3-hydroxypiperidine-4-carboxylate → 8-Benzyl-6-hydroxy-2,8-diazaspiro[4.5]decan-1-one

Participants

Reaction Conditions

Reaction Steps

Into a 10000-mL 3-necked round-bottom flask was placed a solution of ethyl 4-(2-aminoethyl)-1-benzyl-3-hydroxypiperidine-4-carboxylate (220 g, 718.02 mmol, 1.00 equiv) in methanol (2000 mL) and ammonia (2000 mL). The resulting solution was stirred overnight at 45° C. The resulting mixture was concentrated under vacuum. The residue was applied onto a silica gel column and eluted with dichloromethane/methanol to obtain the title compound.

Provenance & Evidence