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Dimethylformamide → 4-Fluoro-3-hydroxy-2-(1-methyl-1-phenylethyl)isoindolinone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dimethylformamide | HCID 6228 | — |
| 反応物 | N,N,N',N'-Tetramethylethylenediamine | HCID 8037 | — |
| 反応物 | 3-fluoro-N-(1-methyl-1-phenylethyl)benzamide | HCID 47444746 | — |
| 反応物 | HCID 178444656 | HCID 178444656 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4-Fluoro-3-hydroxy-2-(1-methyl-1-phenylethyl)isoindolinone | HCID 68493841 | 93.4% |
反応手順
In a similar manner to Step 2 of Example 16, 3-fluoro-N-(1-methyl-1-phenylethyl)benzamide (2.00 g, 7.77 mmol) was dissolved in THF (80 mL), and the solution was treated with TMEDA (3.8 mL, 24.9 mmol), sec-butyllithium-hexane solution (1.01 mol/L, 24.6 mL, 24.9 mmol) and DMF (1.30 mL, 17.1 mmol). The mixture was purified by slurry using diisopropylether to obtain 4-fluoro-3-hydroxy-2-(1-methyl-1-phenylethyl)isoindolinone (2.07 g, yield 93%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07745641B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-676b6febf4b049ebbf0a608d86ca5fbc |
| 出典メモ | uspto-grants-2010_06 |