Trifluoroacetic acid → 5-amino-N-({4-chloro-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}methyl)-1H-indole-2-carboxamide trifluoroacetate

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Reaction Steps

Trifluoroacetic acid (0.5 ml, 6.49 mmol) was added to a suspension of 1,1-dimethylethyl (2-{[({4-chloro-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}methyl)amino]carbonyl}-1H-indol-5-yl)carbamate (0.038 g, 0.066 mmol) in dichloromethane (2 mL). The resulting solution was stirred at RT for 2 h. The solvent was evaporated and the residue was purified by Reverse-Phase HPLC (water/acetonitrile with 0.1% TFA) to give the title compound (0.017 g, 44%) as a white solid. 1H NMR (400 MHz, DMSO-d6): δ ppm 11.85 (s, 1H), 9.57 (br. s., 2H), 9.07 (s, 1H), 7.78 (s, 1H), 7.41-7.57 (m, 5H), 7.32-7.41 (m, 1H), 7.17 (s, 1H), 6.99-7.13 (m, 1H), 4.53 (s, 2H). MS: m/z 469 (M+1).

Provenance & Evidence