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2-Ethynyl-6-methylpyridin-3-amine → (2-(5-Fluoro-pyridin-3-ylethynyl)-6-methyl-pyridin-3-yl)amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Ethynyl-6-methylpyridin-3-amine | HCID 18454776 | — |
| 反応物 | 3-Fluoro-5-iodopyridine | HCID 18454778 | — |
| 触媒 | HCID 178418476 | HCID 178418476 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 生成物 | (2-(5-Fluoro-pyridin-3-ylethynyl)-6-methyl-pyridin-3-yl)amine | HCID 10036674 | 22% |
反応手順
To a solution of Cul (11 mg, 0.06 mmol) in triethylamine (5 ml) were added (2-ethynyl-6-methyl-pyridin-3-yl)amine (40 mg, 0.30 mmol, described in Example 7), (PPh3)2PdCl2 (21 mg, 0.06 mmol), and 3-fluoro-5-iodopyridine (111 mg, 0.45 mmol). The reaction mixture was stirred at room temperature for 14 h. The solvent was evaporated. The crude residue was purified by flash chromatography (cyclohexane/ethyl acetate 7:3) to yield 15 mg (66 μmol, 22%) of (2-(5-fluoro-pyridin-3-ylethynyl)-6-methyl-pyridin-3-yl)amine as a yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07205411B2 |
| 出典データセット | uspto-grants-2007_04 |
| ORD ID | ord-bf9e5549b426412f821840f0bbe51ebc |
| 出典メモ | uspto-grants-2007_04 |