関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Methanol | HCID 887 | — |
| 反応物 | Boron tribromide | HCID 25134 | — |
| 反応物 | Ethyl 2-(3-fluoro-4-methoxyphenyl)cyclopropanecarboxylate | HCID 58566289 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 2-[3-Fluoro-4-hydroxy-phenyl]-cyclopropanecarboxylic acid ethyl ester | HCID 58566707 | 91.3% |
反応手順
After 2-(3-fluoro-4-methoxy-phenyl)-cyclopropanecarboxylic acid ethyl ester (0.494 g, 2.07 mmol) obtained in Step B was dissolved in anhydrous DCM (7 mL), BBr3 1 M DCM solution (3 mL, 3.11 mmol) was added thereto at −78° C., and the mixture was stirred at room temperature for 3 hours. After the termination of the reaction, the reactant was added with MeOH, concentrated under reduced pressure, and purified by column chromatography (eluent, EtOAc/Hex=1/2) to obtain the title compound (0.424 g, 91%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09447044B2 |
|---|
| 出典データセット | uspto-grants-2016_09 |
|---|
| ORD ID | ord-e91ce22eda65405f81aff1bdb27a793d |
|---|
| 出典メモ | uspto-grants-2016_09 |
|---|
