関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | 2,5-Dibromopyridine | HCID 69353 | — |
| 反応物 | 2,4-Difluorophenylboronic acid | HCID 2734334 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 5-Bromo-2-(2,4-difluorophenyl)pyridine | HCID 57461242 | 84% |
反応手順
One 1.0 L round bottom flask was charged with 2,5-dibromopyridine (10.45 g, 44.1 mmol); (2,4-difluorophenyl) boronic acid (7.66 g, 48.5 mmol); potassium carbonate (12.19 g, 88 mmole); diacetoxypalladium (0.495 g, 2.206 mmol); triphenylphosphine (1.157 g, 4.41 mmol); and acetonitrile (348 ml) and MeOH (174 ml). The reaction mixture was heated to 40° C. for 40 hours. The reaction mixture was diluted with deionized water and extracted with ethyl acetate. The organic portion was combined and subjected to column chromatography (SiO2 gel, 10% EtOAc in heptane) to yield the desired compound, 5-bromo-2-(2,4-difluorophenyl)pyridine (10 g; 84%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09450195B2 |
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| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-ebbdbaf6e1da42ebb383ede2836bedf4 |
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| 出典メモ | uspto-grants-2016_09 |
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