戻る
化工社化工社 化学情報印刷レポート · 研究参考用
HRID 466作成日:2026年10月24日

Glycine ethyl ester, hydrochloride → Ethyl 2-[(3-amino-5-fluoro-2-pyridinyl)amino]acetate

https://huagongshe.com/ja/reaction/466

反応式

関与物質

役割名称HCID仕込み量
反応物Glycine ethyl ester, hydrochlorideHCID 2723640—
反応物2-Bromo-5-fluoropyridin-3-amineHCID 40427367—
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 2-[(3-amino-5-fluoro-2-pyridinyl)amino]acetateHCID 1322248480%

反応条件

温度120 °C

反応手順

In a 50 mL round-bottomed flask 2-bromo-5-fluoropyridin-3-amine (500 mg, 2.62 mmol) ethyl 2-aminoacetate hydrochloride (731 mg, 5.24 mmol) BINAP (163 mg, 0.26 mmol) palladium(II) acetate (58.8 mg, 0.26 mmol) CESIUM CARBONATE (2559 mg, 7.85 mmol) were taken.The solids were mixed well and degassed.The toluene was taken in another RB and degassed using Nitrogen.The degassed toluene was then added to the solids.The resulting RM was heated to reflux for 16 hrs. The reaction was monitored by LCMS, which indicated starting material only and no required product. Therefore, the batch was discarded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-a7df51f0be0a4af98f3bfe87d6600255
出典メモ750 AstraZeneca ELN dataset