Zopolrestat → HCID 12071529, compound

Participants

Reaction Steps

To a solution of [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (419 mg, 1.0 mmol) in acetone (20 mL) was added triethanolamine (1.49 g, 10.0 mmol). After stirring at ambient temperature for 1.0 hours, the mixture was evaporated to a semi-solid, which was crystallized from ethanol:acetone (1:4) to afford the title compound as a white crystalline solid (494 mg, 86%). mp: 83-84° C.; 1H NMR (D2O, 350 MHz): δ 3.30 (m, 6H), 3.67 (s, 2H), 3.79 (m, 6H), 5.47 (s, 2H), 7.17 (m, 1H), 7.48-7.71 (m, 5H), 8.01 (m, 1H); MS (Cl) 419 (MH).

Provenance & Evidence