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HRID 387958作成日:2026年10月25日

Dimethylformamide → 4-(4-Amino-3-fluorophenoxy)-7-(1-methylpiperidin-3-ylmethoxy)quinoline-6-carbonitrile

https://huagongshe.com/reaction/387958

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物Potassium CarbonateHCID 11430—
反応物3-Chloromethyl-1-methylpiperidinium chlorideHCID 106690—
反応物4-(4-Amino-3-fluorophenoxy)-6-cyano-7-hydroxyquinolineHCID 135829379—
溶媒WaterHCID 962—
溶媒Ethyl AcetateHCID 8857—
生成物4-(4-Amino-3-fluorophenoxy)-7-(1-methylpiperidin-3-ylmethoxy)quinoline-6-carbonitrileHCID 2293677610.9%

反応条件

温度20 °C

反応手順

After adding dimethylformamide (4 ml), 3-chloromethyl-1-methylpiperidine hydrochloride (621 mg) and potassium carbonate (840 mg) to 4-(4-amino-3-fluorophenoxy)-6-cyano-7-hydroxyquinoline (400 mg), the mixture was stirred at 20° C. for 3 hours. Water was added to the reaction solution, extraction was performed with ethyl acetate, the organic layer was washed with water and saturated saline in that order and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The obtained crude product was purified by NH silica gel column chromatography (ethyl acetate) to obtain the title compound (60 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08372981B2
出典データセットuspto-grants-2013_02
ORD IDord-f2152a86cd90490a9ea71f590a261188
出典メモuspto-grants-2013_02