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HRID 634作成日:2026年10月24日

N-Ethylaniline → 5-bromo-N-ethyl-4-methoxy-N-phenylpyrimidin-2-amine

https://huagongshe.com/ja/reaction/634

反応式

関与物質

役割名称HCID仕込み量
反応物N-EthylanilineHCID 7670—
反応物5-Bromo-2-iodo-4-methoxypyrimidineHCID 84819520—
試薬Sodium 2-methylbutan-2-olateHCID 2733478—
触媒Palladium (II) acetateHCID 4144353—
触媒Bis(adamantan-1-yl)(butyl)phosphaneHCID 11371790—
溶媒TolueneHCID 1140—
生成物5-bromo-N-ethyl-4-methoxy-N-phenylpyrimidin-2-amineHCID 10699869353.74%

反応条件

温度60 °C

反応手順

5-bromo-2-iodo-4-methoxypyrimidine (0.086 g, 0.27 mmol), diacetoxypalladium (2.78 mg, 0.01 mmol), di((3S,5S,7S)-adamantan-1-yl)(butyl)phosphine (8.88 mg, 0.02 mmol) and sodium 2-methylbutan-2-olate (0.033 g, 0.30 mmol) were added to a micro vial. Then N-ethylaniline (0.031 mL, 0.25 mmol) in toluene (1.5 mL) was added to the reaction mixture. The vial was sealed and evacuated and flushed with nitrogen and then stirred at 60°C o/n. LC/MS showed product formation. The reaction mixture was cooled to rt and then filtered over celite. The crude product was diluted with 25 ml of DCM and then washed with sat. NaHCO3 followed by brine. The organic phase was dried over a phase separator and then concentrated to dryness. **No LC/MS data due to database failure over three months and was only saved locally on LC/MS computer and pdf-files seems to be deleted on machine. Not used in further reactions.**

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-8bbed4d3f8cb496989e49be7e55b89ca
出典メモ750 AstraZeneca ELN dataset