Ethanol → HCID 136336871, compound

Participants

Reaction Steps

A mixture of (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylonitrile (920 mg, 1.8 mmol) and hydroxylamine (0.18 mL, 2.7 mmol, 50% wt. in water) in ethanol (2 mL) was heated at reflux for 16 h. The ethanol was removed in vacuo, and dichloromethane and water were added. The aqueous layer was extracted with dichloromethane (2×), and the combined organics were washed with brine, dried (MgSO4) and concentrated. Purification by silica gel chromatography (0 to 70% EtOAc/hexanes) provided 433 mg of the title compound as a pale yellow foam. LCMS: 461 [(M-THP+H)+H]+.

Provenance & Evidence