化工社化工社 化学情報印刷レポート · 研究参考用
3-Bromopyridine → 2-Pyridin-3-yl-7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Bromopyridine | HCID 12286 | — |
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 7-(Trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one | HCID 66801593 | — |
| 触媒 | Copper iodide | HCID 83717 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-Pyridin-3-yl-7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one | HCID 56942731 | 22.1% |
反応手順
Using analogous reaction conditions as described in Example 1, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-16c: 150 mg, 0.698 mmol) was reacted with 3-bromo-pyridine (220 mg, 1.395 mmol), 1,4-dioxane (10 mL), copper iodide (13.29 mg, 0.0698 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (29.33 mg, 0.209 mmol) and potassium phosphate (369.9 mg, 1.745 mmol) to afford the crude product. Purification by column chromatography on silica gel (1.5% methanol in DCM) afforded 45 mg of the product (22.05% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08946260B2 |
| 出典データセット | uspto-grants-2015_02 |
| ORD ID | ord-8f90849e00324bf8939ff1b8d4dd3eea |
| 出典メモ | uspto-grants-2015_02 |