化工社化工社 化学情報印刷レポート · 研究参考用
Dabco → N-(2,4-dimethoxybenzyl)-2,4,5-trifluoro-N-(pyrimidin-4-yl)benzenesulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dabco | HCID 9237 | — |
| 反応物 | 2,4,5-Trifluorobenzenesulfonyl chloride | HCID 2776979 | — |
| 反応物 | N-(2,4-Dimethoxybenzyl)pyrimidin-4-amine | HCID 63362995 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | N-(2,4-dimethoxybenzyl)-2,4,5-trifluoro-N-(pyrimidin-4-yl)benzenesulfonamide | HCID 89556048 | 53% |
反応手順
To a solution of the N-(2,4-dimethoxybenzyl)pyrimidin-4-amine (0.76 g, 3.10 mmol) prepared in Example 14a and 1,4-diazabicyclo[2.2.2]octane (0.70 g, 6.20 mmol) in acetonitrile (20 mL), 2,4,5-trifluorobenzenesulfonyl chloride (1.43 g, 6.20 mmol) was added with cooling on ice, and the reaction solution was stirred at room temperature for 1 hour. The reaction solution was filtered, the filtrate was vacuum concentrated, and the residue was purified with silica gel chromatography (hexane/ethyl acetate=67:33) to yield the title compound (0.72 g, 53%) as a colorless solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08889741B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-cdeb0a4f4650488ba3d96571877ff022 |
| 出典メモ | uspto-grants-2014_11 |