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HRID 341作成日:2026年10月24日

1-Bromo-4-fluorobenzene → 4-(4-Fluorophenyl)piperazin-2-one

https://huagongshe.com/ja/reaction/341

反応式

関与物質

役割名称HCID仕込み量
反応物1-Bromo-4-fluorobenzeneHCID 9993—
反応物Piperazin-2-oneHCID 231360—
試薬Sodium t-butoxideHCID 23676156—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Palladium (II) acetateHCID 4144353—
溶媒TolueneHCID 1140—
生成物4-(4-Fluorophenyl)piperazin-2-oneHCID 534149910%

反応条件

温度150 °C

反応手順

diacetoxypalladium (11.21 mg, 0.05 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (28.9 mg, 0.05 mmol) were dissolved in toluene (0.5 mL) under nitrogen. Stirred at 50C for 30min. sodium 2-methylpropan-2-olate (96 mg, 1.00 mmol) and piperazin-2-one (50 mg, 0.50 mmol) were added to a second microwave vial and inerted with nitrogen. 1-bromo-4-fluorobenzene (0.055 mL, 0.50 mmol) and toluene (0.500 mL) were added. The catalyst solution wad added to the reaction mixture and the resulting solution was stirred at 100C for 1h in the microwave. No reaction. Then 150C for 1h, still no reaction. The reaction was discarded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-cc7dfeae12f6444baf8a8a863fd60e2b
出典メモ750 AstraZeneca ELN dataset