関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 5-Bromo-2-chloropyridine | HCID 2734414 | — |
| 反応物 | Cyclopropylboronic acid | HCID 2760897 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-Chloro-5-cyclopropylpyridine | HCID 50988858 | 57.1% |
反応手順
To a suspension of 5-bromo-2-chloropyridine (990 mg, 5.15 mmol), cyclopropylboronic acid (893 mg, 10.39 mmol) and Cs2CO3 (5.082 g, 15.45 mmol) in 1,4-dioxane (25 mL) was added Pd(PPh3)4 (601 mg, 0.52 mmol) at r.t. under N2. The reaction was stirred at 100° C. for 1 h. After filtration, the solvent was removed in vacuo, and the residue was purified by silica gel chromatography (PE:EtOAc=50:1) to give 452 mg (57%) of the title compound as a colorless oil. [M+H] Calc'd for C8H8NCl, 154. Found, 154.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09447046B2 |
|---|
| 出典データセット | uspto-grants-2016_09 |
|---|
| ORD ID | ord-52ed6b39f3aa48a795435627d53ab571 |
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| 出典メモ | uspto-grants-2016_09 |
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