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HRID 660生成日期:2026年10月23日

间溴三氟甲苯 → [3-(Trifluoromethyl)phenyl](3-methoxyphenyl)amine

https://huagongshe.com/zh-CN/reaction/660

反应方程式

参与物

角色名称HCID投料
反应物间溴三氟甲苯HCID 9817—
反应物间氨基苯甲醚HCID 10824—
试剂叔丁醇钠HCID 23676156—
催化剂4,5-双二苯基膦-9,9-二甲基氧杂蒽HCID 636044—
催化剂醋酸钯HCID 4144353—
溶剂苯甲醚HCID 7519—
产物[3-(Trifluoromethyl)phenyl](3-methoxyphenyl)amineHCID 825370280%

反应条件

温度50 °C

反应步骤

PdOAc2 (8 mg, 0.04 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (40 mg, 0.07 mmol) were added to a dried vial. The vial was caped with a septa-cap and inerted with nitrogen. Degassed anisole (2 mL)was added and the catalyst mixture was heated to 50ºC for 30 minutes, then cooled down to rt. A dry 2ml microwave vial was charged with sodium 2-methylpropan-2-olate (52 mg, 0.54 mmol). It was caped and inerted with nitrogen. A degassed mixture of 1-bromo-3-(trifluoromethyl)benzene (50 µL, 0.36 mmol) and 3-methoxyaniline (50 µL, 0.45 mmol) in anisole (2 mL) wad added at rt. The catalyst solution was added to the reaction mixture. The nitrogen inlet was removed and the vial was inserted into an alumina block at 100°C. The reaction was stirred over night. After 19h, the reaction was cooled down and filtered through celite. The filtrate was concentrated. Large amounts of anisole was present. No product was detected by LCMS. The sample was descarded.

来源与证据

来源数据集750 AstraZeneca ELN dataset
ORD IDord-09a52aa0a68e4624905d84eed602571e
来源说明750 AstraZeneca ELN dataset