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Isobutyronitrile → (alphaS)-3-Fluoro-beta-[[1-(4-fluorophenyl)-1H-indazole-5-yl]oxy]-alpha-(2-methylpropyl)benzeneethanamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Isobutyronitrile | HCID 6559 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 1-(4-fluorophenyl)-5-iodo-1H-indazole | HCID 59251128 | — |
| 反応物 | (2S)-2-Amino-1-(3-fluorophenyl)-4-methyl-pentane-1-ol | HCID 66812540 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 生成物 | (alphaS)-3-Fluoro-beta-[[1-(4-fluorophenyl)-1H-indazole-5-yl]oxy]-alpha-(2-methylpropyl)benzeneethanamine | HCID 66812773 | 23.3% |
反応手順
(2S)-2-Amino-1-(3-fluorophenyl)-4-methyl-pentane-1-ol (350 mg, 1.66 mmol), 5-iodo-1-(4-fluorophenyl)-1H-indazole (672.2 mg, 1.99 mmol), cesiumcarbonate (1.08 g, 3.31 mmol), copper (I)-iodide (157.8 mg, 0.83 mmol) and isobutyronitrile (1.75 mL) are stirred in a glass pressure tube at 120° C. for 20 h. The reaction mixture is filtered via a glass microfibre filter, the solvent evaporated and the residue purified by chromatography (silicagel, eluents: ethylacetate/methanol). 162.8 mg (23.3%) of the title compound are obtained.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07728030B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-2f77677a013141f9a96d85bec8fd7e1c |
| 出典メモ | uspto-grants-2010_06 |