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HRID 557作成日:2026年10月23日

p-Bromoacetophenone → Tert-butyl 4-(4-acetylphenyl)piperazine-1-carboxylate

https://huagongshe.com/ja/reaction/557

反応式

関与物質

役割名称HCID仕込み量
反応物p-BromoacetophenoneHCID 7466—
反応物tert-Butyl piperazine-1-carboxylateHCID 143452—
試薬Cesium carbonateHCID 10796—
触媒Binap, (A+-)-HCID 634876—
触媒Palladium (II) acetateHCID 4144353—
溶媒TolueneHCID 1140—
生成物Tert-butyl 4-(4-acetylphenyl)piperazine-1-carboxylateHCID 2113619052.48%

反応条件

温度120 °C

反応手順

In a CEM MW vial, p-Bromoacetophenone (729 ml, 6.03 mmol),tert-Butyl 1-piperazinecarboxylate (1.684 g, 9.04 mmol),racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (0.375 g, 0.60 mmol),Palladium (II) acetate (0.135 g, 0.60 mmol),Cesium carbonate (3.93 g, 12.06 mmol) was taken in toluene (10 ml).The RM was subjected to MW power of 300W,temp 120°C for 45 minutes. The LCMS was checked showed the formation of required mass. Work-up: The RM was passed through hyflow bed and filtrate was evaporated and chrmatographed using Ethyl acetate hexane to obtain tert-butyl 4-(4-acetylphenyl)piperazine-1-carboxylate (0.963 g, 52.5 %).

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-c7d1825ed35e4dffbc57a0b9b8fa9354
出典メモ750 AstraZeneca ELN dataset