Phosphorus oxychloride → HCID 18393037, compound

Participants

Reaction Steps

To a solution of (2S)-1-acetoxy-3-(3,4-dimethoxyphenyl)-2-{2-[4-(3-pyridyl)phthalazin-1(2H)-on-2-yl]isonicotinoylamino}propane (150 mg) in acetonitrile (5 ml) is added phosphorus oxychloride (0.29 ml), and the mixture is heated under reflux overnight. The reaction mixture is cooled to room temperature, and neutralized with an aqueous sodium hydrogen carbonate solution. The mixture is extracted with chloroform, and the extract is washed, dried, and concentrated. The residue is crystallized from ethyl acetate to give (3S)-4-(3-acetoxymethyl-3,4-dihydro-6,7-dimethoxyisoquinolin-1-yl)-2-[4-(3-pyridyl)phthalazin-1(2H)-on-2-yl]pyridine (136 mg), as yellow crystals.

Provenance & Evidence