1,4-Dioxane hydrochloride → 2,2-dimethyl-5-[3-({[(1R)-1-(1-naphthyl)ethyl]amino}methyl)-4-phenylpiperidin-1-yl]-5-oxopentanoic acid hydrochloride

Participants

Reaction Steps

To 225 mg of the crude 5-[3-({(tert-butoxycarbonyl)[(1R)-1-(1-naphthyl)ethyl]amino}methyl)-4-phenylpiperidin-1-yl]-2,2-dimethyl-5-oxopentanoic acid was added 2.0 mL of a 4 M hydrogen chloride/1,4-dioxane solution 2.0 mL, followed by stirring at room temperature for 1 hour. The reaction mixture was concentrated under reduced pressure, and the residue was then dissolved in THF. Diisopropylether was added dropwise thereto, and the precipitate was isolated by filtration. This was dried under reduced pressure at 50° C. to obtain 170 mg of 2,2-dimethyl-5-[3-({[(1R)-1-(1-naphthyl)ethyl]amino}methyl)-4-phenylpiperidin-1-yl]-5-oxopentanoic acid hydrochloride as a white solid.

Provenance & Evidence