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HRID 241573作成日:2026年10月25日

Acetic Acid → trans-6-(2,5-Difluorophenyl)-1-benzyl-5-nitropiperidin-2-one

https://huagongshe.com/reaction/241573

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物BenzylamineHCID 7504—
反応物Methyl 4-nitrobutyrateHCID 25604—
反応物2,5-DifluorobenzaldehydeHCID 137663—
反応物Sodium AcetateHCID 517045—
溶媒EthanolHCID 702—
生成物trans-6-(2,5-Difluorophenyl)-1-benzyl-5-nitropiperidin-2-oneHCID 67388890—

反応手順

To a solution of 2,5-difluorobenzaldehyde (1.09 g, 7.67 mmol) in ethanol (20 mL) were added methyl 4-nitrobutyrate (1.13 g, 7.04 mmol), benzylamine (0.98 mL, 7.67 mmol), sodium acetate (1.26 g, 15.3 mmol) and acetic acid (0.88 mL, 15.4 mmol). The mixture was stirred at rt for 12 h and then heated at reflux temperature overnight. After evaporation, the residue was purified by column chromatography (silica gel Biotage 40M™) eluting with ethyl acetate/hexane (gradient from 3% to 50%) to give the title compound as the racemic trans isomer. LC-MS: 347.1 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08653059B2
出典データセットuspto-grants-2014_02
ORD IDord-9c81f34126db454a9c58bf2b4af6f2ab
出典メモuspto-grants-2014_02