Zopolrestat → HCID 12071528, compound

Participants

Reaction Steps

To a solution of [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (2.09 g, 5.0 mmol) in acetone (200 mL) was added diethanolamine (1.05 g, 10.0 mmol). After stirring at ambient temperature for 2.0 hours, the mixture was evaporated to a semi-solid, which was crystallized from ethanol:acetone (1:5) to afford the title compound as a white crystalline solid (2.12 g, 81%). mp: 163-164° C.; 1H NMR (D2O, 350 MHz): δ 3.05 (m, 4H), 3.61 (s, 2H), 3.69 (m, 4H), 5.42 (s, 2H), 7.03 (m, 1H), 7.35 (m, 1H), 7.48-7.65 (m, 4H), 7.92 (m, 1H); MS (Cl) 419 (MH+).

Provenance & Evidence