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Iodo benzene diacetate → N-(5-((2-aminopyridin-4-yl)oxy)pyridin-2-yl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Iodo benzene diacetate | HCID 12217721 | — |
| 反応物 | 4-((6-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamido)pyridin-3-yl)oxy)picolinamide | HCID 73053266 | — |
| 反応物 | EtOAc CH3CN water | HCID 86658869 | — |
| 生成物 | N-(5-((2-aminopyridin-4-yl)oxy)pyridin-2-yl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide | HCID 73053627 | 77% |
反応手順
To a solution of 4-((6-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamido)pyridin-3-yl)oxy)picolinamide (60 mg, 0.13 mmol) in EtOAc/MeCN/H2O (2 mL/2 mL/1 mL) was added iodobenzene diacetate (54 mg, 0.16 mmol) at 0° C. The reaction was stirred at rt for 2 hours, then concentrated in vacuo. The resulted residue was dissolved in EtOAc (10 mL), washed with saturated aq. NaHCO3, and then dried over anhydrous Na2SO4. The organic solution was concentrated in vacuo to give the title compound as a yellow solid (43 mg, 77%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08975282B2 |
| 出典データセット | uspto-grants-2015_03 |
| ORD ID | ord-69c0f0e0fab1401fb64d181061d6c418 |
| 出典メモ | uspto-grants-2015_03 |