Water → 1-[4-(2-Chloro-4-fluoro-benzoyl)-piperidin-1-yl]-ethanone

Participants

Reaction Conditions

Reaction Steps

2-Chloro-4-fluoro-1-iodobenzol (5 g, 19 mmol) was solved in THF (3 mL) and at −10° C. isopropyl magnesium chloride-lithium chloride (2M in THF) was added dropwise and the mixture stirred for 30 minutes at 0° C. At −10° C. 1-acetyl-isonipecotoyl chloride was added (3.3 g, 18 mmol) solved in THF (2 mL) and the mixture stirred for 10 minutes to −10° C. and 4 h to 0° C. Water was added and the reaction extracted with dichloromethane. Chromatography with Heptane/EtOAc (2:1) gave the desired compound as a clear orange liquid (1.8 g, 33% yield). (m/e): 284.3 (M+H+).

Provenance & Evidence