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HRID 1108208作成日:2026年10月27日
Potassium Iodide → 5-Fluoro-3-(1-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}piperidin-4-ylmethyl)-1H-indole
https://huagongshe.com/reaction/1108208
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Iodide | HCID 4875 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 1-(2-Chloroethyl)-4-(2-methoxyphenyl)piperazine | HCID 595673 | — |
| 反応物 | 5-fluoro-3-[(4-piperidinyl)methyl]-1H-indole | HCID 11287716 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 5-Fluoro-3-(1-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}piperidin-4-ylmethyl)-1H-indole | HCID 9825015 | 80% |
反応手順
Pulverized potassium carbonate (0.76 g, 5.5 mmole) and potassium iodide (0.97 g, 5.5 mmole) was added to a mixture of 4-(5-fluoro-1H-indol-3-ylmethyl)piperidine (1.16 g, 5.0 mmole) and 1-(2-chloroethyl)-4-(2-methoxyphenyl)piperazine (1.27 g, 5.0 mmole) in 25 ml of acetonitrile. The resulting mixture was heated to reflux under nitrogen for 5 hours. After cooling, it was diluted with water (150 ml) and the product extracted into ethyl acetate (50 ml). The organic layer was washed with water (50 ml), brine (50 ml), and after drying over sodium sulfate, filtration and concentration in vacuo afforded the required product as a white solid (1.8 g, 80%). Treatment with an excess of 1M etheral hydrochloric acid gave the acid addition salt, which was recrystallized from methanol.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06066637 |
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| 出典データセット | uspto-grants-2000_05 |
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| ORD ID | ord-c57ffb01e9a7445d9a831e48cdd8bab1 |
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| 出典メモ | uspto-grants-2000_05 |
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