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Potassium Carbonate → Ziprasidone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Sulfolane | HCID 31347 | — |
| 反応物 | 3-(1-Piperazinyl)-1,2-benzisothiazole | HCID 2772144 | — |
| 反応物 | 5-(2-Chloroethyl)-6-chlorooxindole | HCID 10609474 | — |
| 触媒 | Potassium Iodide | HCID 4875 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | Ziprasidone | HCID 60854 | 74.8% |
反応手順
In glass-lined reactor placed 21.1 Kg (96.34 mole) of 3-piperazinylbenzo[d]isothiazole; 31 kg (134.7 moles) of 6-chloro-5-(2-chloroethyl)indolin-2-one; 1.1 kg of potassium iodide; 20.0 kg (111.92 mole) of potassium carbonate and 63.2 lit of sulfolane. The contents of the flask were initially heated to 75° C. to 80° C. for 2 hrs. Then temperature was raised to 95° C. to 100° C. and stirred till completion of the reaction. After completion of the reaction 210 lit of DM water was added to the reaction mixture and stirred. The product was filtered off and washed with water and dried to obtain 29.75 kg of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one (Ziprasidone).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07728136B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-1f25ff321e514b58b4c5fca27a5d1686 |
| 出典メモ | uspto-grants-2010_06 |