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Hydrochloric Acid → 3-Fluoro-4-methoxyphenylboronic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | Triisopropyl borate | HCID 21531 | — |
| 反応物 | 4-Bromo-2-fluoroanisole | HCID 75378 | — |
| 反応物 | Magnesium | HCID 5462224 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 3-Fluoro-4-methoxyphenylboronic acid | HCID 2782194 | 78.6% |
反応手順
Then, 9.6 g of magnesium was added to 230 ml of THF, and the solution thus formed was slowly added dropwise with 70.9 g of the 4-bromo-2-fluoroanisole obtained by the procedure mentioned above to prepare a Grignard reagent. The reagent was added dropwise to a mixture of 123.8 g of triisopropyl borate and 391 ml of THF at a temperature of -60° C. to -50° C. with stirring. After the dropping of the reagent was finished, the solution was subjected to reaction at an ambient temperature for 2 hours, added with 242 ml of a 1N-aqueous hydrochloric acid solution, subjected to further reaction for 1 hour, extracted with an ether, washed with water, and concentrated under a reduced pressure to obtain 46.2 g of 4-methoxy-3-fluorobenzene boronic acid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05417885 |
| 出典データセット | uspto-grants-1995_05 |
| ORD ID | ord-25b0f0e5e9c241c398e5745d30c58bb2 |
| 出典メモ | uspto-grants-1995_05 |