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HRID 454866作成日:2026年10月26日

1,2-Dimethoxyethane → 6-Chloro-1-(4-fluoro-2-methylphenyl)phthalazine

https://huagongshe.com/reaction/454866

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DimethoxyethaneHCID 8071—
反応物Sodium CarbonateHCID 10340—
反応物(4-Fluoro-2-methylphenyl)boronic acidHCID 2734665—
反応物1,6-DichlorophthalazineHCID 14322333—
触媒HCID 178418476HCID 178418476—
溶媒EthanolHCID 702—
溶媒MethanolHCID 887—
生成物6-Chloro-1-(4-fluoro-2-methylphenyl)phthalazineHCID 66739677—

反応条件

温度80 °C

反応手順

A mixture of 1,6-dichlorophthalazine (5.39 g, 27.1 mmol), 4-fluoro-2-methylphenylboronic acid (5.00 g, 32.5 mmol), trans-dichlorobis(triphenylphosphine)palladium (II) (0.950 g, 1.35 mmol), and sodium carbonate (8.61 g, 81.2 mmol) in a 2:1 mixture of DME and EtOH (40 mL) was heated at 80° C. in an oil bath for 18 h. The mixture was cooled to room temperature, diluted with MeOH and filtered through a pad of Celite. The filtrate was concentrated over silica gel and purified using column chromatography (0-25% EtOAc in hexanes) to provide the title compound as a yellow crystalline solid. MS (ESI, pos. ion) m/z: 272.8 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08497269B2
出典データセットuspto-grants-2013_07
ORD IDord-e58d42084b4e4f40a7c92999a1b40f21
出典メモuspto-grants-2013_07