反应详情

温度

50 °C

To a solution of 2,2,2-trifluoro-N-[(3-{[4-(2-{3-[(2-thienylacetyl)amino]phenyl}-pyrazolo[1,5-a]pyridin-3-yl)-2-pyrimidinyl]amino}phenyl)methyl]acetamide (71 mg, 0.11 mmol) in THF (3 mL) was added LiOH hydrate (10 mg, 0.21 mmol) in water (0.5 mL). The solution was heated to 50° C. for 2 h, and then diluted with DCM, washed with 1N Na2CO3, dried over Na2SO4, and concentrated to generate the title compound in 94% yield. 1H NMR (400 MHz, d6-DMSO) 610.37 (s, 1H), 9.51 (s, 1H), 8.83 (d, J=6.8 Hz, 1H), 8.53 (d, J=8.8 Hz, 1H), 8.24 (d, J=5.4 Hz, 1H), 7.90 (s, 1H), 7.74-7.76 (m, 2H), 7.55 (d, J=8.1 Hz, 1H), 7.38-7.50 (m, 3H), 7.28 (d, J=7.5 Hz, 1H), 7.19 (t, J=7.8 Hz, 1H), 7.12 (t, J=6.8 Hz, 1H), 6.94-6.98 (m, 3H), 6.46 (d, J=5.3 Hz, 1H), 3.88 (s, 2H), 3.67 (s, 2H). ES-LC/MS m/z=532 [M+H]+.

1. washwashed with 1N Na2CO3
2. dry with materialdried over Na2SO4
3. concentrationconcentrated