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HRID 476作成日:2026年10月24日

5-Bromo-2-fluorotoluene → Methyl N-(4-fluoro-3-methylphenyl)piperidine-4-carboxylate

https://huagongshe.com/ja/reaction/476

反応式

関与物質

役割名称HCID仕込み量
反応物5-Bromo-2-fluorotolueneHCID 123527—
反応物Methyl isonipecotateHCID 424914—
試薬Sodium t-butoxideHCID 23676156—
触媒Binap, (A+-)-HCID 634876—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物Methyl N-(4-fluoro-3-methylphenyl)piperidine-4-carboxylateHCID 590233660%

反応条件

温度110 °C

反応手順

In a 100 mL round-bottomed flask methyl piperidine-4-carboxylate (2.2 g, 15.36 mmol),4-bromo-1-fluoro-2-methylbenzene (1.954 mL, 15.36 mmol),Pd2(dba)3 (0.521 g, 0.57 mmol),BINAP (0.574 g, 0.92 mmol) and sodium tert-butoxide (4.43 g, 46.09 mmol) was taken in toluene (10 mL) under N2.The resulting reaction was stirred at 110 °C for 3 hrs. LCMS did not show product MS.Material was discrded.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-498c0c75d66a47609408cbfbddaef8e5
出典メモ750 AstraZeneca ELN dataset