HCID 66783258, compound → HCID 44602502, compound

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Reaction Steps

A solution of (S)-1-{3-[(S)-4-(tert-butyl-dimethyl-silanyloxy)-6-aza-spiro[2.5]oct-6-yl]-propyl}-4-(3-chloro-4-trifluoromethyl-phenyl)-3-methyl-piperazin-2-one (65 mg, 0.11 mmol) and hydrogen fluoride pyridine complex (70% HF; 0.26 mL) in CH3CN (3 mL) was heated at 50° C. for 16 h, then partitioned between EtOAc and sat. aq. NaHCO3 solution. The organic layer was washed with brine, dried (MgSO4), filtered, and evaporated. Chromatography (IST Isolute® Flash NH2; EtOAc-MeOH gradient) afforded the title compound (29 mg, 56%) in a diastereomeric ratio of 97:3. Colourless gum, MS: 460.3 (M+H)+.

Provenance & Evidence