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HRID 475作成日:2026年10月23日

1,4-Dibromobenzene → Methyl 2-(4-(4-bromophenyl)piperazin-1-yl)acetate

https://huagongshe.com/ja/reaction/475

反応式

関与物質

役割名称HCID仕込み量
反応物1,4-DibromobenzeneHCID 7804—
反応物1-Piperazineacetic acid, methyl esterHCID 15343158—
試薬Cesium carbonateHCID 10796—
触媒Binap, (A+-)-HCID 634876—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒1,4-DioxaneHCID 31275—
生成物Methyl 2-(4-(4-bromophenyl)piperazin-1-yl)acetateHCID 580645200%

反応条件

温度85 °C

反応手順

In a reaction vial, 1,4-dibromobenzene (0.373 g, 1.58 mmol), methyl 2-(piperazin-1-yl)acetate (0.100 g, 0.63 mmol), CS2CO3 (0.309 g, 0.95 mmol), and BINAP (0.024 g, 0.04 mmol) were taken up in 1,4-dioxane (1.5 ml). Argon was bubbled through the solution for 1 minute. Pd2(dba)3 (0.012 g, 0.01 mmol) was added, followed by additional purging with argon. The vial was capped and placed on the heater-shaker. The reaction was stirred (450 rpm) at 100 °C overnight. LC/MS at this point did not indicate any formation of the dp. Experiment not progressed.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-cf737b8f3d9340aca6130b04f75e7c21
出典メモ750 AstraZeneca ELN dataset