化工社化工社 化学情報印刷レポート · 研究参考用
Potassium Phosphate, Tribasic → 2-(5-Fluoro-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 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 3-Bromo-5-fluoropyridine | HCID 820206 | — |
| 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-(5-Fluoro-pyridin-3-yl)-7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one | HCID 66807324 | 27.19% |
反応手順
Using analogous reaction conditions as described in Example 1, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-16c: 90 mg, 0.419 mmol) was reacted with 3-bromo-5-fluoro-pyridine (73.67 mg, 0.419 mmol), 1,4-dioxane (10 mL), copper iodide (7.98 mg, 0.0419 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (17.85 mg, 0.126 mmol) and potassium phosphate (222 mg, 1.048 mmol) to afford the crude product. Purification by column chromatography on silica gel (0.5% methanol in DCM) afforded 35 mg of the product (27.19% 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-1d82c553e1ec4bf286dd41da411a7f39 |
| 出典メモ | uspto-grants-2015_02 |