Trimethylphosphine → 1-[5-Chloro-8-(3-fluorophenyl)isoquinolin-7-yl]ethanamine

Participants

Reaction Steps

To a stirred mixture of 7-(1-azidoethyl)-5-chloro-8-(3-fluorophenyl)isoquinoline (0.105 g, 0.321 mmol) in tetrahydrofuran (2 mL) and water (0.4 mL) was added 1.0 M trimethylphosphine in THF (0.39 mL, 0.39 mmol). The mixture was stirred at room temperature for 1 hour. After nitrogen was passed through the reaction solution, the reaction mixture was extracted with dichloromethane. The extracts were washed with brine, dried over magnesium sulfate and evaporated to dryness. The crude residue was used directly in the next step (75 mg, 78%). LCMS calculated for C17H15ClFN2 (M+H)+: m/z=301.1; Found: 301.1.

Provenance & Evidence