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4-(piperazin-1-yl)-1H-indole → 1-(4-Fluoro-phenoxy)-3-[4-(1H-indol-4-yl)piperazin-1-yl]-propan-2-ol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(piperazin-1-yl)-1H-indole | HCID 594590 | — |
| 反応物 | 2-[(4-Fluorophenoxy)methyl]oxirane | HCID 2724792 | — |
| 生成物 | 1-(4-Fluoro-phenoxy)-3-[4-(1H-indol-4-yl)piperazin-1-yl]-propan-2-ol | HCID 9842266 | 99.3% |
反応手順
A methanolic solution (50 ml) of 1-(4-fluorophenoxy)-2,3-epoxypropane (0.50 g, 3.0 mmole) and 1-(indol-4-yl)-piperazine (0.6 g, 3.0 mmole) was refluxed for 1 hr under an atmosphere of nitrogen. The mixture was concentrated in vacuo, and the product purified by silica gel chromatography (EtOAc) to afford a white solid (1.1 g, 99%). Treatment with a 0.25M ethanolic fumaric acid solution gave the required salt, which was recrystallized from ethanol to afford the title compound as a white solid. m.p. 234-235° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06689792B2 |
| 出典データセット | uspto-grants-2004_02 |
| ORD ID | ord-e857271eeb2d4d52a14e3a6007374227 |
| 出典メモ | uspto-grants-2004_02 |