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Acetyl chloride → Abiraterone Acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Acetyl chloride | HCID 6367 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Abiraterone | HCID 132971 | — |
| 反応物 | Triethylazanium chloride | HCID 12698378 | — |
| 触媒 | 2-Dimethylaminopyridine | HCID 21885 | — |
| 溶媒 | Diethyl Ether | HCID 3283 | — |
| 生成物 | Abiraterone Acetate | HCID 9821849 | 84.3% |
反応手順
To a stirred suspension of finely powdered 17-(3-pyridyl)androsta-5,16-dien-3β-ol (3.50 g, 10 mmol) in dry diethyl ether (150 ml) coning triethylamine (2,3 ml, 16 mmol) and dimethylaminopyridine (0.012 g, 0.1 mmol) was added acetyl chloride (1.0 ml, 14 mmol). The mixture was then stirred at ambient temperature for 12 h, over which time a thick whim precipitate of triethylammonium chloride had formed. The mixture was then filtered and the filtrate concentrated to afford the crude product which was recrystallised firstly from ethanol/water (1:1), then finally from hexane to afford the title compound (3.30 g, 84%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05618807 |
| 出典データセット | uspto-grants-1997_04 |
| ORD ID | ord-94d92c56bf574920853a00aa70205454 |
| 出典メモ | uspto-grants-1997_04 |