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HRID 584作成日:2026年10月23日

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

https://huagongshe.com/ja/reaction/584

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105 °C

反応手順

In a 100 mL round-bottomed flask (t=g) was methyl 2-bromoisonicotinate (.5 g, 2.31 mmol), 4-fluoro-N-methylaniline (0.348 g, 2.78 mmol), and CS2CO3 (1.056 g, 3.24 mmol) in toluene (16 mL) to give a yellow suspension. Pd2dba3 (0.106 g, 0.12 mmol) and biphenyl-2-yldicyclohexylphosphine (0.122 g, 0.35 mmol) were added. Reaction was allowed to stir overnight. LC/MS in the morning revealed little product had formed. Something with mass 272 dominated. Reaction was discarded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-3a62166a30464afb9cbe502b267cbcba
出典メモ750 AstraZeneca ELN dataset