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HRID 13567作成日:2026年10月25日

Potassium Carbonate → Ziprasidone

https://huagongshe.com/reaction/13567

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物SulfolaneHCID 31347—
反応物3-(1-Piperazinyl)-1,2-benzisothiazoleHCID 2772144—
反応物5-(2-Chloroethyl)-6-chlorooxindoleHCID 10609474—
触媒Potassium IodideHCID 4875—
溶媒WaterHCID 962—
生成物ZiprasidoneHCID 6085474.8%

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US07728136B2
出典データセットuspto-grants-2010_06
ORD IDord-1f25ff321e514b58b4c5fca27a5d1686
出典メモuspto-grants-2010_06