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Potassium Carbonate → Aripiprazole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 7-(4-Chlorobutoxy)-1,2,3,4-tetrahydroquinolin-2-one | HCID 10467467 | — |
| 反応物 | 1-(2,3-Dichlorophenyl)piperazine hydrochloride | HCID 11630372 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | Aripiprazole | HCID 60795 | 75.1% |
反応手順
Potassium carbonate (8.39 g) was dissolved in water (140 mL), followed by the addition of 7-(4-chlorobutoxy)-3,4-dihydrocarbostyril (19.4 g) and 1-(2,3-dichlorophenyl)piperazine monohydrochloride (16.2 g) thereto. The mixture was refluxed under stirring for about 3 hours. After reaction, the resulting mixture was cooled, and precipitated crystals were filtered. The crystals were dissolved in ethyl acetate (350 mL), and about 210 mL of water/ethyl acetate azeotrope was distilled under reflux. The remaining solution was cooled, and precipitated crystals were filtered. The thus-obtained crystals were dried at 60° C. for 14 hours, thereby obtaining 20.4 g of crude aripiprazole (yield: 74.2%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09278934B2 |
| 出典データセット | uspto-grants-2016_03 |
| ORD ID | ord-947a69e652f144cfabd426ecae67b4fd |
| 出典メモ | uspto-grants-2016_03 |