Trimethylpyruvic acid → HCID 57344121, compound

Participants

Reaction Steps

4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one TFA salt (320 mg, 0.65 mmol), 3,3-dimethyl-2-oxobutanoic acid [1.6 g (60%), 7.39 mmol], DIPEA (3 ml, 17.4 mmol), and HATU (1.5 g, 3.92 mmol) were mixed in DMF (50 ml). After the resulting reaction mixture was stirred at room temperature for 87 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 preparative TLC (EA:PE=1:1) to afford the desired product (30 mg, 9.1%) as an off white solid.

Provenance & Evidence