(Diethylamino)sulfur trifluoride → HCID 73057751, compound

Participants

Reaction Conditions

Reaction Steps

A suspension of 3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one (55.8 mg, 0.20 mmol) in dichloromethane (0.5 ml) is cooled to −78° C. Diethylaminosulfurtrifluoride (105 μl, 0.80 mmol) is added. The reaction mixture is allowed to reach room temperature within 30 minutes (formation of a clear solution). The reaction mixture is evaporated and the residue is treated with water and saturated sodium hydrogen carbonate solution. The solids are filtered off and chromatographed on a silica gel column with cyclohexane/ethyl acetate as eluent to afford 3-[4-(1-fluoro-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one as fine white powder; HPLC/MS 1.94 min (A), [M+H] 282;

Provenance & Evidence