(R)-8-(2-chloro-1-methylethyl)-8-azaspiro[4.5]decane-7,9-dione → 8-{(1R)-2-[4-(2,5-Difluorophenyl)piperazin-1-yl]-1-methylethyl}-8-azaspiro[4.5]decane-7,9-dione

Participants

Reaction Conditions

Reaction Steps

A mixture of 1-(2,5-difluorophenyl)piperazine (20 mg, 0.10 mmol) and (R)-8-(2-chloro-1-methylethyl)-8-azaspiro[4.5]decane-7,9-dione (20 mg, 0.082 mmol) was heated with stirring at 160° C. for 5 hours. The residue was purified by preparative HPLC [reverse phase column (C18 HC), water/methanol (70:30) with 0.1% TFA to water/methanol (40:60) with 0.1% TFA gradient, UV detection at λ254 nm or λ215 nm], giving (after removal of the solvent) the title compound as a pale yellow oil (21.5 mg, 0.05 mmol, 66%): ESI-MS m/z 406 (MH+).

Provenance & Evidence