Water → HCID 10248990, compound

Participants

Reaction Steps

Compound 14 (50 mg, 0.14 mmol) is dissolved in DMF (0.15 mL) and Hunig's base is added (0.048 mL, 0.27 mmol) followed by 4-chlorobenzyl chloride (22 mg, 0.14 mmol) at room temperature. The reaction is stirred for 1 hour and then water (0.2 mL) is added and the resulting solids are filtered and washed with water and then methylene chloride to provide 3-(4-Chloro-benzylsuIfanyl)-5-(pyridin-3-ylamino)-isothiazole-4-carboxylic acid amide (25.7 mg, 49%). 1H NMR (d6 DMSO): δ 10.37 (1H, br. s), 8.51 (1H, d, J=2.8 Hz), 8.26 (1H, d, J=4.4 Hz), 7.61–7.64 (1H, m), 7.42 (2H, d, J=8 Hz), 7.38–7.41 (1H, m), 7.33 (2H, J=8 Hz), 4.40 (2H, s). LRMS (M+): 376.9, (M−): 374.9.

Provenance & Evidence