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Dimethylformamide → 4,7-Dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dimethylformamide | HCID 6228 | — |
| 反応物 | 2,5-dichloro-N-(1-methyl-1-phenylethyl)nicotinamide | HCID 86628338 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4,7-Dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one | HCID 86628339 | 72% |
反応手順
In a similar manner to Step 2 of Example 16, 2,5-dichloro-N-(1-methyl-1-phenylethyl)nicotinamide (400 mg, 1.29 mmol) was dissolved in THF (16 mL), and the solution was treated with n-butyllithium-hexane solution (2.71 mol/L, 1.20 mL, 3.23 mmol) and DMF (0.250 mL, 3.23 mmol), followed by purification by slurry (diisopropylether) and flash column chromatography (hexane/ethyl acetate=60/40 to 50/50) to obtain 4,7-dichloro-1-hydroxy-2-(1-methyl-1-phenylethyl)-1,2-dihydropyrrolo[3,4-c]pyridine-3-one (312 mg, yield 72%).
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-9b31b26df4874decaa6523a04b293c68 |
| 出典メモ | uspto-grants-2010_06 |