Phthalimide → HCID 86681476, compound

Participants

Reaction Steps

To a solution of 6-chloro-2-[(1S)-1-(3,5-difluorobenzyl)-2-hydroxyethyl]-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one (0.340 g, 1.00 mmol), triphenylphosphine (0.263 g, 1.00 mmol) and phthalimide (0.148 g, 1.00 mmol) in tetrahydrofuran (10 mL) at 25° C. was added diethyl azodicarboxylate (0.514 mL, 1.30 mmol). The reaction was stirred at room temperature overnight. After concentration, the residue was purified by combi-flash chromatography eluting with EtOAc/hexane (10-60%). The purification gave 0.360 g (76.7% yield) of the desired product as light green solid. LC/MS found: 468.0 (M+1)+.

Provenance & Evidence