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HRID 81628作成日:2026年10月26日
Dimethylacetamide → 6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine
https://huagongshe.com/reaction/81628
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Dimethylacetamide | HCID 31374 | — |
| 反応物 | 4-[(1-Methyl-1H-pyrazol-3-yl)amino]quinazolin-6-ol | HCID 23160382 | — |
| 反応物 | Potassium tert-butoxide | HCID 23665647 | — |
| 反応物 | 2-(2,2-Diethoxyethoxy)-5-fluoropyrimidine | HCID 68427683 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | 6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine | HCID 68428853 | 37.6% |
反応手順
2-(2,2-Diethoxyethoxy)-5-fluoropyrimidine (168 mg, 0.73 mmol) and potassium tert-butoxide (93 mg, 0.83 mmol) were added to an N,N-dimethylacetamide solution (1 ml) of 4-[(1-methyl-1H-pyrazol-3-yl)amino]quinazolin-6-ol (80 mg, 0.33 mmol), and stirred at 190° C. for 14 hours under a nitrogen atmosphere in a sealed tube. The reaction solution was cooled with ice, water was added, and extracted with chloroform. The organic layer was washed with water, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (Moritex, acetone:hexane=1:2) to obtain 6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine (56 mg, yield: 37%) as a pale brown amorphous solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08846700B2 |
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| 出典データセット | uspto-grants-2014_09 |
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| ORD ID | ord-d1e59b377485443ca7fa41e9f0b25ca9 |
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| 出典メモ | uspto-grants-2014_09 |
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