8-[2-(6,6-Dimethyl-bicyclo[3.1.1]hept-2-yl)-ethyl]-3-(3-methylamino-propyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one → 4-{[(3-{8-[2-(6,6-Dimethyl-bicyclo(3.1.1]hept-2-yl)-ethyl]-4-oxo-1-phenyl-1,3,8-triaza-spiro[4.5]dec-3-yl} propyl)-methyl-amino]-methyl}-4-hydroxy-piperidine-1-carboxylic Acid Tert-Butyl Ester

Participants

Reaction Steps

2.6 g (5.74 mmol) of compound (24) was placed in a flask and diluted with 20 ml ethanol. To this solution was added 1.88 g (8.81 mmol) of the epoxide (32) and the mixture was heated to reflux until TLC showed complete conversion. For work-up the solvent was evaporated and the residue was taken up with ethyl acetate. After washing with aqueous potassium carbonate solution drying over sodium sulphate and concentration in vacuo the raw material was purified via flash column chromatography yielding a light yellow viscous oil (3.51 g, 5.15 mmol, 89.8% yield).

Provenance & Evidence