関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Phenylpropanolamine | HCID 10297 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 5-iodo-1-isopropyl-1H-indazole | HCID 59339864 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 溶媒 | Butyronitrile | HCID 8008 | — |
| 生成物 | (1R,2S)-1-[(1-isopropyl-1H-indazol-5-yl)oxy]-1-phenylpropan-2-amine | HCID 59339639 | — |
反応手順
A mixture of 5-iodo-1-isopropyl-1H-indazole (30c, 461 mg, 1.26 mmol), (1R,2S)-2-amino-1-phenylpropan-1-ol (286 mg, 1.89 mmol), copper (I) iodide (25 mg, 130 μmol), and cesium carbonate (1.45 g, 3.8 mmol) in butyronitrile (5 ml) was stirred at 125° C. for 2 h. Then the mixture was cooled to room temp., the inorganic material was removed by filtration and washed with ethyl acetate. The combined organic solutions were concentrated i. vac., and the product purified by flash chromatography on silica gel (ethyl acetate/methanol). Yield 200 mg (51%) of a brown oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08030340B2 |
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| 出典データセット | uspto-grants-2011_10 |
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| ORD ID | ord-92984ab5255a42178e20c7dc7fd750c4 |
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| 出典メモ | uspto-grants-2011_10 |
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