関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Indole | HCID 798 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 1,4-Dioxane | HCID 31275 | — |
| 反応物 | Methylboronic Acid | HCID 139377 | — |
| 触媒 | Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+) | HCID 178418228 | — |
| 生成物 | 4,5-dimethyl-1H-indole-3-carboxylic acid | HCID 57057416 | 91.8% |
反応手順
A mixture of bromide 1 (1.0 g, 4.78 mmol), methyl boronic acid (860 mg, 14.3 mmol), Pd(dppf)2Cl2 (194 mg, 0.239 mmol), and K2CO3 (1.32 g, 9.56 mmol) in dioxane (20 mL) was degassed and stirred at 90° C. for 5 h under nitrogen. The reaction mixture was concentrated, and the residue was purified by silica gel chromatography (EtOAc/petroleum ether=1/4) to give the desired product (636 mg, 4.39 mmol, 91.8%) as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09434724B2 |
|---|
| 出典データセット | uspto-grants-2016_09 |
|---|
| ORD ID | ord-bc86db76d4f148378e7240faa3b5a944 |
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| 出典メモ | uspto-grants-2016_09 |
|---|
