反应详情

A solution of] (4-{3-Methoxy-4-[7-(2-methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-phenyl}-piperidin-1-yl)-acetic acid tert-butyl ester (73 mg, 0.13 mmol) in 2 mL of 4N HCl in dioxane was stirred at RT. After 18 h, solvent was evaporated and the mixture was triturated with ether. A solid was obtained which was filtered, washed with ether (twice) and dried. The product, (4-{3-Methoxy-4-[7-(2-methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-phenyl}-piperidin-1-yl)-acetic acid was isolated as a pale yellow hygroscopic solid (54 mg, 82%). LCMS (E/I+) 488 (M+H). NMR 1H (DMSO-d6)-10.1 (br s, 1H), 8.96 (s, 1H0, 8.05 (d, 1H, J=8.24 Hz), 7.81 (d, 1H, J=7.49 Hz), 7.68 (s, 1H), 7.46 (m, 1H), 7.41 (d, 1H, J=7.96 Hz), 7.21 (d, 1H, J=8.34 Hz), 7.11 (d, 1H, J=7.45 Hz), 7.08 (m, 1H), 6.98 (m, 2H), 6.70 (d, 1H, J=7.32 Hz), 4.16 (br s, 2H), 4.05-3.1 (series of m and s along with the water peak, 10H), 2.8 (m, 1H), 2.03 (m, 4H).

1. customsolvent was evaporated
2. customthe mixture was triturated with ether
3. customA solid was obtained which
4. filtrationwas filtered
5. washwashed with ether (twice) and
6. customdried