Ammonia → HCID 90040127, compound

Participants

Reaction Steps

To a suspension of 7-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one (149 mg, 0.50 mmol) and sodium azide (71.5 mg, 1.10 mmol) in dichloromethane (1 ml) is added a solution of trifluoroacetic acid (316 μl, 4.1 mmol) in dichloromethane (0.5 ml) dropwise under external cooling with ice. The reaction mixture is stirred for 2 hours at room temperature. Water and 25% aqueous ammonia (0.5 ml) are added. The organic phase is separated and the aqueous phase is extracted with dichloromethane. The combined organic phases are dried over sodium sulfate and evaporated to afford 3-[4-(1-azido-1-methyl-ethyl)-phenyl]-7-fluoro-2H-isoquinolin-1-one as white powder; HPLC/MS 2.07 min (A), [M+H] 323.

Provenance & Evidence