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HRID 1959525作成日:2026年10月27日

Potassium Carbonate → {3-[5-Amino-1-(5-cyclopropylcarbamoyl-2-methyl-phenyl)-1H-pyrazole-4-carbonyl]-phenoxy}-acetic acid

https://huagongshe.com/reaction/1959525

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物tert-Butyl chloroacetateHCID 66052—
反応物3-[5-amino-4-(3-hydroxy-benzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamideHCID 11245836—
溶媒DimethylformamideHCID 6228—
生成物{3-[5-Amino-1-(5-cyclopropylcarbamoyl-2-methyl-phenyl)-1H-pyrazole-4-carbonyl]-phenoxy}-acetic acidHCID 5808894130.4%

反応条件

温度100 °C

反応手順

To a stirred solution of 3-[5-amino-4-(3-hydroxy-benzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide (400 mg, 1.06 mmol) and t-butyl chloroacetate (319 mg, 2.12 mmol) in DMF (20 mL) was added K2CO3 (292 mg, 2.12 mmol) and the mixture was heated at 100° C. overnight. The solvent was removed, and the residue was suspended in EtOAc, washed by water, brine, dried over Na2SO4, and concentrated. The crude product was purified by column chromatography on silica gel (EtOAc:Hexane=3:1) to provide the product as a light yellow oil (140 mg, 27%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08410160B2
出典データセットuspto-grants-2013_04
ORD IDord-a0e6e2b138f6495aa0d75334c672fb21
出典メモuspto-grants-2013_04