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HRID 166作成日:2026年10月24日

2-Chloro-4-aminopyrimidine → (3-(2-Chloropyrimidin-4-ylamino)-4-fluorophenyl)methanol

https://huagongshe.com/ja/reaction/166

反応式

関与物質

役割名称HCID仕込み量
反応物2-Chloro-4-aminopyrimidineHCID 345752—
反応物3-Bromo-4-fluorobenzyl AlcoholHCID 2773351—
試薬Cesium carbonateHCID 10796—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,4-DioxaneHCID 31275—
生成物(3-(2-Chloropyrimidin-4-ylamino)-4-fluorophenyl)methanolHCID 598178450%

反応条件

温度150 °C

反応手順

diacetoxypalladium (8.67 mg, 0.04 mmol) was added to 2-chloropyrimidin-4-amine (100 mg, 0.77 mmol), (3-bromo-4-fluorophenyl)methanol (158 mg, 0.77 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (53.6 mg, 0.09 mmol) and cesium carbonate (503 mg, 1.54 mmol) in 1,4-dioxane (4 mL) . The resulting suspension was stirred at 150 °C in the microwave for 30 minutes. None of the desired material was visible by LCMS. Reaction abandoned.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-99e222e4d9a34b6bb8073fb91a88f0f7
出典メモ750 AstraZeneca ELN dataset