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HRID 420605作成日:2026年10月25日

Citric Acid → 4-(2-Hydroxyethyl)-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrile

https://huagongshe.com/reaction/420605

反応式

関与物質

役割名称HCID仕込み量
反応物Citric AcidHCID 311—
反応物Tetramethylammonium fluorideHCID 67803—
反応物4-[2-(t-Butyldimethyl silyloxy)ethyl]-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrileHCID 57966452—
生成物4-(2-Hydroxyethyl)-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrileHCID 5796656795%

反応条件

温度0 °C

反応手順

To 4-[2-(t-butyldimethyl silyloxy)ethyl]-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrile (510 mg) was added tetramethylammonium fluoride (1 M tetrahydrofuran solution, 1.63 mL). The mixture was stirred at 0° C. for 0.5 hour. To the reaction solution was added aqueous citric acid solution and extracted with ethyl acetate. The organic layer was washed with water and brine, and dried over sodium sulphate. The solvent was evaporated under reduced pressure and the residue was purified by column chromatograph on silica gel to give the title compound (366 mg). Yield: 95%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08097610B2
出典データセットuspto-grants-2012_01
ORD IDord-3f30962b45294306898de9dec91c9712
出典メモuspto-grants-2012_01