Sulfamic Acid → HCID 25164927, compound

Participants

Reaction Conditions

Reaction Steps

4-Formyl-N-{2-oxo-2-[4-(2-trifluoromethyl-benzoyl)-piperazin-1-yl]-ethyl}-benzamide (40 mg, 0.90 mmol) was dissolved in an acetone-water mixture (1:1, 0.9 mL) and cooled to 0° C. A mixture of sulphamic acid (26 mg, 0.27 mmol) and sodium chlorite (32 mg, 0.36 mmol) dissolved in minimum amount of water was then added. The resulting mixture was allowed to warm to room temperature and stirred for 30 minutes. 5 mL of water was then added, and the product was extracted with ethyl acetate. The organic layer was washed with brine solution, dried over sodium sulphate and concentrated to afford 25 mg (61% yield) of N-{2-Oxo-2-[4-(2-trifluoromethyl-benzoyl)-piperazin-1-yl]-ethyl}-terephthalamic acid. LCMS Purity: 95.8%, 1H NMR (DMSO-d6): δ 13 (bs, 1H). 8.8 (m, 1H), 8.1-7.9 (m, 4H), 7.9-7.8 (m, 1H), 7.8-7.7 (m, 1H), 7.7 (m, 1H), 7.6-7.5 (m, 1H), 4.3-4.1 (m, 4H), 3.6-3.4 (m, 8H).

Provenance & Evidence