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Potassium Carbonate → Buspirone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 8-Azaspiro(4.5)decane-7,9-dione | HCID 136843 | — |
| 反応物 | 8-Aza-5-azoniaspiro(4.5)decane, 8-(2-pyrimidinyl)-, bromide (1:1) | HCID 657505 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | Buspirone | HCID 2477 | — |
反応手順
A mixture 3,3-tetramethyleneglutarimide (16.7 g., 0.1 mole) , 8-(2-pyrimidinyl)-8-aza-5-azoniaspiro[4.5]decane bromide (29.9 g., 0.1 mole) and potassium carbonate (16.6 g., 0.12 mole) in 190 ml. of dimethylformamide is maintained at 150°-155° C. for a reaction period of 24 hours and then evaporated to dryness under reduced pressure. The resulting solid is triturated with 90 ml. of water, taken up in 10% hydrochloric acid and filtered. The acid filtrate is made basic with 10% aqueous sodium hydroxide and precipitated free base collected and dried to provide 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04351939 |
| 出典データセット | uspto-grants-1982_09 |
| ORD ID | ord-83befe68e5e54d4fb6cbccca0da4d085 |
| 出典メモ | uspto-grants-1982_09 |