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HRID 585作成日:2026年10月24日

4-Fluoro-N-methylaniline → methyl 2-(4-fluoro-N-methylanilino)pyridine-4-carboxylate

https://huagongshe.com/ja/reaction/585

反応式

関与物質

役割名称HCID仕込み量
反応物4-Fluoro-N-methylanilineHCID 68024—
反応物2-Bromo-isonicotinic acid methyl esterHCID 3847768—
試薬Cesium carbonateHCID 10796—
触媒2-(Dicyclohexylphosphino)biphenylHCID 2734216—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物methyl 2-(4-fluoro-N-methylanilino)pyridine-4-carboxylateHCID 1083792060%

反応条件

温度85 °C

反応手順

In a 100 mL round-bottomed flask (t=g) was biphenyl-2-yldicyclohexylphosphine (0.024 g, 0.07 mmol), methyl 2-bromoisonicotinate (.1 g, 0.46 mmol), and 4-fluoro-N-methylaniline (0.070 g, 0.56 mmol) in toluene (3 mL) to give a purple suspension. Pd2dba3 (0.021 g, 0.02 mmol) and CS2CO3 (0.211 g, 0.65 mmol) were added. Flask was placed in an oil bath at 85 °C. LC/MS taken at 1, 2 and 4 hours indicated reaction was not progressing. Reaction was discarded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-8fdcadcf8d694b72a4ad9ff8119e3e79
出典メモ750 AstraZeneca ELN dataset