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Pyridine → 1-(4-Fluorophenyl)-5-iodo-6-methylindazole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | 4-Fluorophenylboronic acid | HCID 285645 | — |
| 反応物 | 5-iodo-6-methyl-1H-indazole | HCID 59339696 | — |
| 触媒 | Cupric acetate | HCID 8895 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 1-(4-Fluorophenyl)-5-iodo-6-methylindazole | HCID 59339914 | 51.1% |
反応手順
5-Iodo-6-methylindazole (1.3 g, 5.0 mmol), p-fluorobenzeneboronic acid (1.4 g, 10 mmol), anhydrous copper(II) acetate (1.4 g, 7.5 mmol) and pyridine (0.80 mL, 10 mmol) were stirred in dichloromethane (30 mL) overnight. Additional portions of p-fluorobenzeneboronic acid (0.47 g, 3.4 mmol), anhydrous copper(II) acetate (0.45 g, 2.5 mmol) and pyridine (0.27 mL, 3.4 mmol) were added. The mixture was filtered through celite after stirring for an additional night. The filtrate was concentrated and purified by column chromatography (SiO2, toluene) to give the subtitle compound (0.90 g, 51%) as a light orange powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07728030B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-72bb574897744091b253023ce7c3b848 |
| 出典メモ | uspto-grants-2010_06 |