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HRID 510879作成日:2026年10月26日

Water → Methyl 3'-acetyl-5'-chloro-3-fluoro-2'-methoxy-6'-methylbiphenyl-4-carboxylate

https://huagongshe.com/reaction/510879

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物3-Fluoro-4-(methoxycarbonyl)benzeneboronic acidHCID 2782818—
反応物1-(3-Bromo-5-chloro-2-methoxy-4-methylphenyl)ethanoneHCID 86666759—
触媒HCID 178418397HCID 178418397—
溶媒Sodium CarbonateHCID 10340—
溶媒1,4-DioxaneHCID 31275—
生成物Methyl 3'-acetyl-5'-chloro-3-fluoro-2'-methoxy-6'-methylbiphenyl-4-carboxylateHCID 86666801—

反応条件

温度100 °C

反応手順

A mixture of 1-(3-bromo-5-chloro-2-methoxy-4-methylphenyl)ethanone (1.0 g, 3.6 mmol) and [3-fluoro-4-(methoxycarbonyl)phenyl]boronic acid (0.85 g, 4.3 mmol) in 1,4-dioxane (12 mL) and 10% sodium carbonate in water (5.73 mL, 5.40 mmol) was bubbled with N2 to degas. After tetrakis(triphenylphosphine)palladium(0) (166 mg, 0.144 mmol) was added, the mixture was bubbled with N2 for 5 min. more and heated at 100° C. overnight. The mixture was cooled to room temperature and diluted with ethyl acetate. The layers were separated and the aq. layer was extracted with more ethyl acetate. The combined extracts were washed with brine, dried over Na2SO4, filtered, and concentrated to give crude product.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09096600B2
出典データセットuspto-grants-2015_08
ORD IDord-b74237beef2345269d14478eb90f3d6b
出典メモuspto-grants-2015_08