5-Aminosalicylic Acid → HCID 66800045, compound

Participants

Reaction Steps

A solution of 5-chloro-3-methyl-benzo[b]thiophene-2-sulfonyl chloride (22 mg, 0.075 mmol) and 5-aminosalicylic acid (17 mg, 0.112 mmol) in aqueous dioxane (800 μL, 4:1 dioxane/water) was shaken at 35° C. for 5 days. The product was purified by reversed phase chromatography (ACE C8, 4 μm, 21×50 mm, flow 25 ml/min, gradient: 0.1% TFA in water/MeCN over 6 minutes). The title compound was obtained in 79% yield (23.6 mg). 1H NMR (500 MHz, DMSO-d6) δ ppm 2.41-2.43 (m, 3 H) 6.87 (d, J=8.79 Hz, 1 H) 7.20-7.25 (m, 1 H) 7.53 (dd, J=2.93, 1.46 Hz, 1 H) 7.56 (dd, J=8.79, 1.95 Hz, 1 H) 8.00 (d, J=1.95 Hz, 1 H) 8.06 (d, J=8.79 Hz, 1 H) 10.45 (s, 1 H). MS (ESI+) m/z 398 [M+H]+.

Provenance & Evidence