Acetonitrile → HCID 59201237, compound

Participants

Reaction Conditions

Reaction Steps

2-(Fluorosulphonyl)difluoroacetic acid (0.040 ml, 0.385 mmol) was added to a stirred solution/suspension of methyl {(2S,4R)-1-[(1R)-1-(hydroxymethyl)-4-methylpentyl]-2-[4-(trifluoromethyl)phenyl]piperidin-4-yl}acetate (Example 29, Step 1, 160 mg, 0.385 mmol) and Na2SO4 (11 mg, 0.077 mmol) in dry CH3CN (1 ml) at RT under N2. The reaction was then stirred and heated at 50° C. After 2 hours, the reaction was allowed to cool to RT, then partitioned between DCM/H2O. The aqueous layer was extracted with DCM (×2). The combined extracts were dried (Na2SO4), filtered and evaporated. The residue was purified by chromatography (silica, 4-6-10% EtOAc/isohexanes) to give the title compound (13 mg) as an oil. M/Z 466 (MH+).

Provenance & Evidence