反应 #57145

反应方程式

[3-(4-{[(phenylamino)carbonyl]amino}phenyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]acetic acid

1-ethyl-3-(3-dimethylaminopropyl)carbodiimide

m-anisidine

→

title compound

收率 26.0%

N-[3-(methyloxy)phenyl]-2-[3-(4-{[(phenylamino)carbonyl]amino}phenyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]acetamide

收率 26.0%

溶剂

N,N-dimethylformamide

反应条件

后处理

1. 1
   浓缩concentrated in vacuo
2. 2
   洗涤washed with saturated aqueous sodium bicarbonate (10 mL)
3. 3
   干燥The organic layer was dried over sodium sulfate
4. 4
   浓缩concentrated in vacuo
5. 5
   其他Purification by Gilson reverse phase HPLC

实验过程

To a solution of [3-(4-{[(phenylamino)carbonyl]amino}phenyl)-4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]acetic acid (0.166 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (0.249 mmol), 4-dimethylaminopyridine (0.249 mmol) and N,N-dimethylformamide (3.2 mL) at room temperature was added m-anisidine (0.415 mmol). The reaction mixture was stirred overnight at room temperature, concentrated in vacuo, taken up in ethyl acetate (10 mL) and washed with saturated aqueous sodium bicarbonate (10 mL). The organic layer was dried over sodium sulfate and concentrated in vacuo. Purification by Gilson reverse phase HPLC afforded the title compound as a white solid (26%). ESMS [M+H]+: 558.4

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