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HRID 515作成日:2026年10月23日

tert-Butyl carbamate → tert-butyl N-(3-fluoro-5-methyl-2-pyridinyl)carbamate

https://huagongshe.com/ja/reaction/515

反応式

関与物質

役割名称HCID仕込み量
反応物tert-Butyl carbamateHCID 77922—
反応物2-Chloro-3-fluoro-5-methylpyridineHCID 13541365—
試薬Cesium carbonateHCID 10796—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,4-DioxaneHCID 31275—
生成物tert-butyl N-(3-fluoro-5-methyl-2-pyridinyl)carbamateHCID 9006479825.74%

反応条件

温度100 °C

反応手順

diacetoxypalladium (15.42 mg, 0.07 mmol) and(9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (39.8 mg, 0.07 mmol) were added to a degassed mixture of 2-chloro-3-fluoro-5-methylpyridine (100 mg, 0.69 mmol), tert-butyl carbamate (121 mg, 1.03 mmol) and cesium carbonate (336 mg, 1.03 mmol) in dioxane (10 mL) at 21°C. The resulting mixture was stirred at 100 °C for 16 hours.Filtered through celite and adsorbed onto silica. The crude product was purified by flash silica chromatography, elution gradient 0 to 50% DCM in heptane. Pure fractions were evaporated to dryness to afford sm by HNMR Abandoned. ..

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-e2551fd8964c4f0a80ff232c25d61d8a
出典メモ750 AstraZeneca ELN dataset