Hydrochloric Acid → HCID 44599409, compound

Participants

Reaction Steps

Sodium hydride (60% in mineral oil, 72 mg, 1.8 mmol) was added to 2-pyrrolidinone (380 mg, 4.5 mmol) in tetrahydrofuran (2.0 mL) under an atmosphere of Argon. The reaction mixture was stirred for 30 minutes at room temperature. To this mixture, 3-bromomethyl-8-fluoro-1-oxo-2-pyridin-3-yl-1,2-dihydro-isoquinoline-4-carboxylic acid[(S)-cyclopropyl-(3-fluoro-phenyl)-methyl]-amide (118 mg, 0.23 mmol) in tetrahydrofuran (5 mL) was added dropwise. The reaction mixture was stirred for 1 hour at room temperature. The reaction mixture was poured into 25 mL 0.2N HCl (aq). The mixture was extracted with ethyl acetate (25 mL). The organic phase was washed with brine, dried over MgSO4 and concentrated in vacuo. The title compound was isolated by preparative TLC on silica gel (eluent: ethyl acetate).

Provenance & Evidence