2-Furylglyoxylic acid → HCID 57344130, compound

Participants

Reaction Steps

4-(3-((1S,4S)-2,5-diazabicyclo[2,2,1]heptane-2-carbonyl)-4-fluorobenzyl)phthalazin-1 (2H)-one TFA salt (200 mg, 0.41 mmol), 2-(furan-2-yl)-2-oxoacetic acid (352 mg, 2.52 mmol), DIPEA (0.63 ml, 3.78 mmol), and HATU (320 mg, 0.84 mmol) were mixed in DMF (30 ml). After the resulting reaction mixture was stirred at room temperature for 60 h, the reaction mixture was partition between DCM and water (100 ml each). The aqueous phase was extracted with DCM (100 ml), and the combined organic phase was washed with water, sat. aqueous sodium bicarbonate, and brine, dried over sodium sulphate, filtered, and concentrated to yield the crude product. Then the crude product was purified by column chromatography on silica gel (Petroleum ether:Ethyl Acetate=1:3) to afford the desired product (106 mg, 50.5%) as a light yellow solid.

Provenance & Evidence