関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 5-iodo-1-pyridin-3-yl-1H-indazole | HCID 59786571 | — |
| 反応物 | 2-Amino-1-[6-methoxypyridin-3-yl]propan-1-ol | HCID 59786583 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 溶媒 | Butyronitrile | HCID 8008 | — |
| 生成物 | 1-[6-Methoxypyridin-3-yl]-1-[1-(pyridin-3-yl)indazol-5-yl]oxypropan-2-amine | HCID 59786580 | — |
反応手順
5-Iodo-1-(3-pyridinyl)indazole (750 mg, 2.3 mmole), 2-Amino-1-[6-methoxypyridin-3-yl]propan-1-ol (410 mg, 2.2 mmol), copper(I)iodide (42 mg, 0.22 mmol) and caesium carbonate (1.45 g, 4.5 mmole) were suspended in butyronitrile (2.4 mL) and toluene (4.8 mL). The reaction vessel was capped and the mixture was stirred at 130° C. for 20 hours. Then the solvent was removed i.vac., and the product purified by chromatography on silica gel. Yield 254 mg (3 0%) as a racemic mixture of two diastereomeres.
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-394ddf0596ae4f78ab2d49184cb624cf |
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| 出典メモ | uspto-grants-2011_10 |
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