関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Sodium Iodide | HCID 5238 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1H-Pyrazol-3-amine, 5-methyl- | HCID 93146 | — |
| 反応物 | 2,4-Dichloro-6-phenylpyrimidine | HCID 241554 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (2-chloro-6-phenyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine | HCID 178418761 | 62.1% |
反応手順
To a solution of 2,4-dichloro-6-phenyl-pyrimidine (300 mg, 1.33 mmol) and 3-amino-5-methylpyrazole (129 mg, 1.33 mmol) in DMF (7 mL) is added triethylamine (195 μL, 1.40 mmol) followed by sodium iodide (200 mg, 1.33 mmol) and the reaction mixture is stirred for 15 hours at 90° C. The resulting solution is partitioned between ethyl acetate and water and the organic phase washed with brine, dried over MgSO4 then concentrated in vacuo. The residue is triturated in methanol and the resulting white solid collected by filtration to afford (2-chloro-6-phenyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine (236 mg, 62%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06653301B2 |
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| 出典データセット | uspto-grants-2003_11 |
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| ORD ID | ord-b73ffd7c7f50478aab6098e63cb4d484 |
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| 出典メモ | uspto-grants-2003_11 |
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