Trifluoroacetic acid → Cyclopropanesulfonic acid [4-(2-fluoro-4-iodo-phenylamino)-6-methoxy-1H-indazol-5-yl]-amide

Participants

Reaction Steps

A solution of 5-cyclopropanesulfonylamino-4-(2-fluoro-4-iodo-phenylamino)-6-methoxy-indazole-1-carboxylic acid tert-butyl ester (217 mg, 0.36 mmol) in DCM (5 mL) was treated with TFA (2 mL) and the reaction mixture stirred at room temperature for 1 hour. The reaction mixture was concentrated in vacuo and the residue triturated with diethyl ether to give the title compound as an off-white solid (102 mg, 52%). LCMS (method A): RT=10.17 [M+H]+=503. 1H NMR (DMSO-d6, 400 MHz): 12.92 (1 H, s), 8.72 (1 H, s), 7.60-7.52 (2 H, m), 7.34-7.24 (2 H, m), 6.71 (1 H, s), 6.53 (1 H, t, J=8.80 Hz), 3.84 (3 H, s), 2.53-2.46 (1 H, m), 0.84-0.73 (2 H, m), 0.72-0.66 (2 H, m).

Provenance & Evidence