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Styrene Oxide → 1-(2-hydroxy-2-phenyl-ethyl)-4-(6-fluoro-1-methyl-1H-indazol-3-yl)-piperidine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Styrene Oxide | HCID 7276 | — |
| 反応物 | 6-Fluoro-1-methyl-3-(piperidin-4-yl)-1H-indazole | HCID 14032608 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 1-(2-hydroxy-2-phenyl-ethyl)-4-(6-fluoro-1-methyl-1H-indazol-3-yl)-piperidine | HCID 18998823 | 33% |
反応手順
A mixture of 4-(6-fluoro-1-methyl-1H-indazol-3-yl)piperidine (1 g; 4.3 mmol) and phenyloxirane (0.6 g; 5 mmol) in 10 ml acetonitrile was refluxed for 16 h. The cooled reaction mixture was concentrated in vacuo and purified by chromatography on silica gel 60 with ethyl acetate: methanol (9:1, v/v) as eluent. Concentration of the appropriate fractions gave 500 mg (33%) of 1-(2-hydroxy-2-phenyl-ethyl)-4-(6-fluoro-1-methyl-1H -indazol-3-yl)-piperidine.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05478845 |
| 出典データセット | uspto-grants-1995_12 |
| ORD ID | ord-57e9edea1081492480bb53605c9388f9 |
| 出典メモ | uspto-grants-1995_12 |