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Potassium Phosphate, Tribasic → 2-(4-cyclopropylpyridin-3-yl)-3,4-dihydrobenzo[4,5]thieno[3,2-c]pyridin-1(2H)-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 | 3,4-Dihydro-[1]benzothieno[3,2-c]pyridin-1(2H)-one | HCID 20074905 | — |
| 反応物 | 4-Cyclopropyl-3-iodopyridine | HCID 66801887 | — |
| 触媒 | Copper iodide | HCID 83717 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-(4-cyclopropylpyridin-3-yl)-3,4-dihydrobenzo[4,5]thieno[3,2-c]pyridin-1(2H)-one | HCID 56941128 | 29.8% |
反応手順
3,4-Dihydro-2H-benzo[4,5]thieno[3,2-c]pyridin-1-one (I-9d: 100 mg, 0.491 mmol) was reacted with 4-cyclopropyl-3-iodo-pyridine (I-73c: 133 mg, 0.65 mmol), 1,4-dioxane (3 mL), copper iodide (9.31 mg, 0.049 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (6.9 mg, 0.049 mmol) and potassium phosphate (313.3 mg, 1.47 mmol) to afford the crude product. Purification by column chromatography on silica gel (1% methanol in CHCl3) afforded 46.8 mg of the product (29.8% 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-26eafa15bb9642e2b2d6b8584e44e57b |
| 出典メモ | uspto-grants-2015_02 |