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HRID 922167作成日:2026年10月25日

Potassium Carbonate → Aripiprazole

https://huagongshe.com/reaction/922167

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7-(4-Chlorobutoxy)-1,2,3,4-tetrahydroquinolin-2-oneHCID 10467467—
反応物1-(2,3-Dichlorophenyl)piperazine hydrochlorideHCID 11630372—
溶媒WaterHCID 962—
生成物AripiprazoleHCID 6079575.1%

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US09278934B2
出典データセットuspto-grants-2016_03
ORD IDord-947a69e652f144cfabd426ecae67b4fd
出典メモuspto-grants-2016_03