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1-(1-Methyl-4-piperidinyl)piperazine → 5-Cyano-3-(2-ethoxypyridin-3-yl)-6-fluoro-2-oxo-2,3-dihydro-1H-indol-3-yl 4-(1-methylpiperidin-4-yl)piperazine-1-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-(1-Methyl-4-piperidinyl)piperazine | HCID 566324 | — |
| 反応物 | Phenyl 5-cyano-3-(2-ethoxypyridin-3-yl)-6-fluoro-2-oxo-3-phenoxycarbonyloxy-2,3-dihydroindole-1-carboxylate | HCID 67087492 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 5-Cyano-3-(2-ethoxypyridin-3-yl)-6-fluoro-2-oxo-2,3-dihydro-1H-indol-3-yl 4-(1-methylpiperidin-4-yl)piperazine-1-carboxylate | HCID 67087686 | 57% |
反応手順
A mixture of 291 mg (0.53 mmol) of phenyl 5-cyano-3-(2-ethoxypyridin-3-yl)-6-fluoro-2-oxo-3-phenoxycarbonyloxy-2,3-dihydroindole-1-carboxylate, 289 mg (1.58 mmol) of 1-(1-methylpiperidin-4-yl)piperazine and 6 ml of dried tetrahydrofuran (THF) was stirred at room temperature overnight. The reaction mixture was concentrated under reduced pressure and stirred with methanol. The precipitated solid was filtered off and dried in a vacuum drying oven. 158 mg of the title compound were obtained as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09434713B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-54e74598eef943ddb12802e8cefb8ffa |
| 出典メモ | uspto-grants-2016_09 |