Sodium hydride → HCID 86685978, compound

Participants

Reaction Steps

To a solution of 2-(5-amino-pyridin-3-yl)-6-chloro-3,4-dihydro-2H-isoquinolin-1-one (27.3 mg, 0.1 mmol, example 15) in dry DMF (2 mL) was added at 0° C. NaH (3.0 mg, 0.12 mmol). The reaction mixture was allowed to stir at room temperature for 5 min before isobutyryl chloride (12.7 mg, 0.12 mmol) was added into the reaction mixture. The reaction mixture was stirred for additional 1 hour and then poured into ice-water and extracted with EtOAc (2×5 mL). The organic layer was dried over anhy. Na2SO4, filtered and concentrated in vacuo to give a crude product which was then purified by prep-HPLC to give title compound (8.1 mg, 24%) as a white solid. MS: 344.1 (M+H+).

Provenance & Evidence