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HRID 607作成日:2026年10月24日

Morpholine → Ethyl 3-morpholinobenzoate

https://huagongshe.com/ja/reaction/607

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物Ethyl 3-bromobenzoateHCID 90488—
試薬Cesium carbonateHCID 10796—
触媒Binap, (A+-)-HCID 634876—
触媒Palladium (II) acetateHCID 4144353—
溶媒TolueneHCID 1140—
生成物Ethyl 3-morpholinobenzoateHCID 714839979.84%

反応条件

温度100 °C

反応手順

A mixture of ethyl 3-bromobenzoate (0.070 mL, 0.44 mmol), cesium carbonate (427 mg, 1.31 mmol), diacetoxypalladium (4.90 mg, 0.02 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (5.44 mg, 8.73 µmol) and morpholine (0.042 mL, 0.48 mmol) in toluene (2 mL) was refluxed for 1h. The reaction mixture was cooled and filtered through celite. The celite was washed with EtOAc. The solvent was removed under reduced pressure. The residue was purified by automated flash chromatography on a SNAP 25 g column. A gradient from 0% to 50% of EtOAc in Heptane over 10CV was used as mobile phase. The product was collected using the wavelength 254 nm.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-0fa3456b7ef04add84c9ed9afa8e014e
出典メモ750 AstraZeneca ELN dataset