1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 66922870, compound

Participants

Reaction Steps

To a solution of {4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]phenyl}acetic acid (Intermediate 5) (0.13 g, 0.34 mmol) in DCM/DMF (1:1, 6 ml) were added EDCI (0.07 g, 0.36 mmol), DMAP (0.004 g, 0.03 mmol) followed by the addition of tert-butyl 2-methylalaninate (Intermediate 8) (0.057 g, 0.36 mmol). The mixture was stirred at RT for overnight. The reaction mixture was diluted with EtOAc (20 ml), washed with water (2×20 ml), brine (20 ml), dried (MgSO4), filtered and concentrated under reduced pressure to leave a yellow oil. Purification by column chromatography (100% EtOAc) afforded the title compound as an off-white solid (78 mg, 44% yield).

Provenance & Evidence