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HRID 49033作成日:2026年10月24日

Potassium Carbonate → 8-{2-[4-(2-Fluoro-phenyl)-piperazin-1-yl]-ethyl}-8-aza-spiro[4.5]decane-7,9-dione

https://huagongshe.com/ja/reaction/49033

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物8-Azaspiro(4.5)decane-7,9-dioneHCID 136843—
反応物1-(2-Chloroethyl)-4-(2-fluorophenyl)piperazineHCID 22074917—
溶媒DimethylformamideHCID 6228—
生成物8-{2-[4-(2-Fluoro-phenyl)-piperazin-1-yl]-ethyl}-8-aza-spiro[4.5]decane-7,9-dioneHCID 986432540.3%

反応手順

A mixture of 3,3-tetramethylene glutarimide (6.9 mg) and potassium carbonate (40 mg) in dimethylformamide (0.5 mL) was stirred at room temperature for 30 minutes. 1-(2-Chloroethyl)-4-(2-fluorophenyl)piperazine (10.0 mg) was added and the resulting solution was heated at 120° C. for 3 hours. The solvent was removed and the residue was purified by thin-layer chomatography (silica gel, eluting with hexane/ethyl acetate, 1:1), giving the title compound as a white solid (6.2 mg, 40%). 1H NMR (300 MHz, CDCl13) δ7.07-6.87 (m, 4H), 3.96 (t, 2H, J=6.6 Hz), 3.05 (t, 4H, J=4.8 Hz), 2.67 (t, 4H, J=4.7 Hz), 2.59 (s, 4H), 2.54 (t, 4H, J=6.6 Hz), 1.73-1.68 (m, 4H), 1.55-1.50 (m, 4H). ESI-MS m/z 374 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06706716B2
出典データセットuspto-grants-2004_03
ORD IDord-689b1f30332f48c19fcaf0451b5e9fe2
出典メモuspto-grants-2004_03