反应详情

Using similar reaction conditions as described in step-iii of example-1, N-(5-(3-(1-(3-fluorobenzyl)-3,5-dimethyl-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-methoxy phenyl)ethane sulfonamide (200 mg, 0.291 mmol) was hydrolyzed by lithium hydroxide (36 mg, 0.87 mmol) in THF/Methanol/Water (10/3/2 ml) to give 25 mg (16.5% yield) after purification by flash chromatography. 1H NMR (DMSO-d6, 300 MHz): δ 11.9 (s, 1H), 9.02 (s, 1H), 8.45 (s, 1H), 7.79 (s, 1H), 7.54-7.49 (m, 3H), 7.19-7.0 (m, 4H), 5.33 (s, 2H), 3.86 (s, 3H), 3.06-3.04 (m, 2H0, 2.17-2.13 (d, 6H), 1.27-1.23 (t, 3H). MS: m/z=534.8 (M+1), HPLC: 90.27% (Method-B).

1. customreaction conditions
2. customto give 25 mg (16.5% yield)
3. customafter purification by flash chromatography