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HRID 911182作成日:2026年10月26日

Sodium Carbonate → 4-Phenyl-N-(2-(2-(pyridin-4-yl)phenoxy)pyrimidin-5-yl)phthalazin-1-amine

https://huagongshe.com/reaction/911182

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物1,4-DioxaneHCID 31275—
反応物(Pyridin-4-yl)boronic acidHCID 2734379—
反応物N-(2-(2-bromophenoxy)pyrimidin-5-yl)-4-phenylphthalazin-1-amineHCID 57756263—
触媒HCID 178477754HCID 178477754—
溶媒WaterHCID 962—
溶媒Ethyl AcetateHCID 8857—
生成物4-Phenyl-N-(2-(2-(pyridin-4-yl)phenoxy)pyrimidin-5-yl)phthalazin-1-amineHCID 57756236—

反応手順

In an argon-purged sealed tube, N-(2-(2-bromophenoxy)pyrimidin-5-yl)-4-phenylphthalazin-1-amine (150 mg, 319 μmol), pyridin-4-ylboronic acid (157 mg, 1.27 μmol), Pd(DPPF)Cl2 (47 mg, 64 μmol), sodium carbonate (239 μl, 478 μmol), and 1,4-dioxane (1.60 ml, 319 μmol) were added. The reaction was stirred at RT for 5 min. The tube was sealed and heated to 100° C. for 18 h. After 16 h, the reaction was cooled to RT, diluted with EtOAc and 10 mL of water. The product was extracted into EtOAc. The organic layer was washed with brine, dried over MgSO4, filtered, and concentrated. The product was purified by column chromatography on silica gel using 60:40 DCM:(90:10:1 DCM:MeOH:NH4OH). The resulting light brown solid was dissolved in 15 mL of DCM, the solvent were removed under vacuum, affording the title compound as a light brown solid. MS Calcd for C29H20N6O: [M]+=468. Found: [M+H]+=469.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08022221B2
出典データセットuspto-grants-2011_09
ORD IDord-7e76ce9502554866a04be52d9dd48cb8
出典メモuspto-grants-2011_09