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HRID 914808作成日:2026年10月25日

Dimethyl Sulfoxide → 1-(1-Benzylpiperidin-4-yl)-2-(2-fluorophenyl)ethanone

https://huagongshe.com/reaction/914808

反応式

関与物質

役割名称HCID仕込み量
反応物Dimethyl SulfoxideHCID 679—
反応物TriethylamineHCID 8471—
反応物Oxalyl chlorideHCID 65578—
反応物1-(1-Benzylpiperidin-4-yl)-2-(2-fluorophenyl)ethanolHCID 22248173—
溶媒WaterHCID 962—
溶媒DichloromethaneHCID 6344—
生成物1-(1-Benzylpiperidin-4-yl)-2-(2-fluorophenyl)ethanoneHCID 2224799373%

反応条件

温度-78 °C

反応手順

After dissolving 7.5 ml of oxalyl chloride in 130 ml of dichloromethane, the solution was cooled to −78° C. and a solution of 6.1 ml of dimethylsulfoxide in dichloromethane (20 ml) was added dropwise while stirring. After stirring for 20 minutes, a solution of 13.4 g of 1-(1-benzylpiperidin-4-yl)-2-(2-fluorophenyl)ethanol in dichloromethane (40 ml) was added dropwise. After stirring for 30 minutes, 24 ml of triethylamine was added and the temperature was raised to room temperature. Water was added to the reaction solution, the organic layer was washed with water and saturated brine in that order and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by NH silica gel column chromatography (solvent: n-hexane/ethyl acetate) to obtain the title compound (9.64 g, 73% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07265108B2
出典データセットuspto-grants-2007_09
ORD IDord-319b5e2b99ed41ca846a55bd1ae62ef4
出典メモuspto-grants-2007_09