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HRID 527作成日:2026年10月23日

Ethyl 4-piperidinecarboxylate → Ethyl 1-(6-chloro-4-methyl-3-pyridinyl)piperidine-4-carboxylate

https://huagongshe.com/ja/reaction/527

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl 4-piperidinecarboxylateHCID 70770—
反応物5-Bromo-2-chloro-4-methylpyridineHCID 2734427—
試薬Sodium t-butoxideHCID 23676156—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物Ethyl 1-(6-chloro-4-methyl-3-pyridinyl)piperidine-4-carboxylateHCID 822251330%

反応条件

温度100 °C

反応手順

TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (22.18 mg, 0.02 mmol) was added to a degassed mixture of ethyl piperidine-4-carboxylate (0.105 mL, 0.68 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine)(xantphos) (28.0 mg, 0.05 mmol) and ethyl 1-(6-chloro-4-methylpyridin-3-yl)piperidine-4-carboxylate and sodium 2-methylpropan-2-olate (65.2 mg, 0.68 mmol) in toluene (3 mL). The resulting suspension was stirred at 100 °C for 20 hours under nitrogen. LCMS indicated little reaction so reaction abandoned.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-4d540317a2f04c1c94f4d355d5594da0
出典メモ750 AstraZeneca ELN dataset