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HRID 1108208作成日:2026年10月27日

Potassium Iodide → 5-Fluoro-3-(1-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}piperidin-4-ylmethyl)-1H-indole

https://huagongshe.com/reaction/1108208

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium IodideHCID 4875—
反応物Potassium CarbonateHCID 11430—
反応物1-(2-Chloroethyl)-4-(2-methoxyphenyl)piperazineHCID 595673—
反応物5-fluoro-3-[(4-piperidinyl)methyl]-1H-indoleHCID 11287716—
溶媒WaterHCID 962—
溶媒AcetonitrileHCID 6342—
生成物5-Fluoro-3-(1-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}piperidin-4-ylmethyl)-1H-indoleHCID 982501580%

反応手順

Pulverized potassium carbonate (0.76 g, 5.5 mmole) and potassium iodide (0.97 g, 5.5 mmole) was added to a mixture of 4-(5-fluoro-1H-indol-3-ylmethyl)piperidine (1.16 g, 5.0 mmole) and 1-(2-chloroethyl)-4-(2-methoxyphenyl)piperazine (1.27 g, 5.0 mmole) in 25 ml of acetonitrile. The resulting mixture was heated to reflux under nitrogen for 5 hours. After cooling, it was diluted with water (150 ml) and the product extracted into ethyl acetate (50 ml). The organic layer was washed with water (50 ml), brine (50 ml), and after drying over sodium sulfate, filtration and concentration in vacuo afforded the required product as a white solid (1.8 g, 80%). Treatment with an excess of 1M etheral hydrochloric acid gave the acid addition salt, which was recrystallized from methanol.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06066637
出典データセットuspto-grants-2000_05
ORD IDord-c57ffb01e9a7445d9a831e48cdd8bab1
出典メモuspto-grants-2000_05