Methanesulfonyl chloride → 2-(4-Cyano-3-fluorophenyl)ethyl methanesulfonate

Participants

Reaction Steps

A solution of 2-fluoro-4-(2-hydroxyethyl)benzonitrile (22.5 g, 136 mmol) and MsCl (23.3 g, 205 mmol) in 200 mL of dry DCM was added dropwise TEA (27.5 g, 273 mmol) at 0° C. The resulting mixture was stirred at room temperature overnight before concentrating to dryness. The residue was dissolved in 300 mL of EtOAc and washed with 1 N HCl and brine, dried over anhydrous Na2SO4 and concentrated to afford crude title compound: LC-MS m/z 244 (M+1)+;

Provenance & Evidence