Cyanuric chloride → 1-[(S)-N-(tert-Butoxycarbonyl)-4-fluoro-beta-methyl-L-phenylalanyl]-2-cyanopyrrolidine

Participants

Reaction Steps

To a stirred solution of the product from Step A (91.7 mg, 0.233 mmol) in anhydrous DMF (1 mL) was added cyanuric chloride (86 mg, 0.466 mmol). After stirring at room temperature for 16 h, the reaction was diluted with ethyl acetate. The organic phase was washed sequentially with water, saturated aqueous sodium bicarbonate solution and brine, dried (magnesium sulfate), and concentrated under reduced pressure. Purification by preparative thin layer chromatography (silica, ethyl acetate eluant) afforded the title compound.

Provenance & Evidence