関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | (Pyridin-4-yl)boronic acid | HCID 2734379 | — |
| 反応物 | Methyl 2-bromo-4-fluorobenzoate | HCID 7210837 | — |
| 触媒 | HCID 178418397 | HCID 178418397 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | Methyl 4-fluoro-2-(pyridin-4-yl)benzoate | HCID 46317422 | 59.8% |
反応手順
A mixture of methyl 2-bromo-4-fluorobenzoate (1.5 g), pyridine-4-boronic acid (0.95 g), sodium carbonate (1.0 g), tetrakis(triphenylphosphine)palladium(0) (0.22 g), water (1.5 mL) and DME (9.0 mL) was stirred at 120° C. for 1 hr under microwave irradiation. The reaction mixture was diluted with water, and the mixture was extracted with ethyl acetate. The extract was washed with water and saturated brine, and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane) to give the title compound (0.89 g).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08871766B2 |
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| 出典データセット | uspto-grants-2014_10 |
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| ORD ID | ord-be13d82738e34ca3bba6061f54ec29df |
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| 出典メモ | uspto-grants-2014_10 |
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