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HRID 69442作成日:2026年10月25日

N-methyl-2-pyrrolidone → 2-{4-[(S)-7-(3-Fluoro-propyl)-2,7-diaza-spiro[4.4]non-2-yl]-phenyl}-6-hydroxy-3,4-dihydro-2H-isoquinolin-1-one

https://huagongshe.com/reaction/69442

反応式

関与物質

役割名称HCID仕込み量
反応物N-methyl-2-pyrrolidoneHCID 13387—
反応物Propane, 1-bromo-3-fluoro-HCID 67699—
反応物Sodium BicarbonateHCID 516892—
反応物2-[(S)-4-(2,7-Diaza-spiro[4.4]non-2-yl)-phenyl]-6-hydroxy-3,4-dihydro-2H-isoquinolin-1-oneHCID 68991808—
溶媒WaterHCID 962—
溶媒Ethyl AcetateHCID 8857—
生成物2-{4-[(S)-7-(3-Fluoro-propyl)-2,7-diaza-spiro[4.4]non-2-yl]-phenyl}-6-hydroxy-3,4-dihydro-2H-isoquinolin-1-oneHCID 68990366—

反応条件

温度50 °C

反応手順

A mixture of 2-[(S)-4-(2,7-diaza-spiro[4.4]non-2-yl)-phenyl]-6-hydroxy-3,4-dihydro-2H-isoquinolin-1-one (0.20 g), 1-bromo-3-fluoro-propane (76 mg), sodium hydrogencarbonate (10 mg) and NMP (5 mL) was heated at 50° C. for 15 hours. The reaction mixture was distributed between ethyl acetate and water. The organic phase was dried over magnesium sulfate and concentrated. The raw product was purified by preparative HPLC. In this way the product was obtained with molecular weight 423.54 (C25H30FN3O2); MS (ESI): 424 (M+H+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822495B2
出典データセットuspto-grants-2014_09
ORD IDord-66e9a8fd87d04aea8e26a46ce96c38f2
出典メモuspto-grants-2014_09