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HRID 81628作成日:2026年10月26日

Dimethylacetamide → 6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine

https://huagongshe.com/reaction/81628

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylacetamideHCID 31374—
反応物4-[(1-Methyl-1H-pyrazol-3-yl)amino]quinazolin-6-olHCID 23160382—
反応物Potassium tert-butoxideHCID 23665647—
反応物2-(2,2-Diethoxyethoxy)-5-fluoropyrimidineHCID 68427683—
溶媒WaterHCID 962—
生成物6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amineHCID 6842885337.6%

反応条件

温度190 °C

反応手順

2-(2,2-Diethoxyethoxy)-5-fluoropyrimidine (168 mg, 0.73 mmol) and potassium tert-butoxide (93 mg, 0.83 mmol) were added to an N,N-dimethylacetamide solution (1 ml) of 4-[(1-methyl-1H-pyrazol-3-yl)amino]quinazolin-6-ol (80 mg, 0.33 mmol), and stirred at 190° C. for 14 hours under a nitrogen atmosphere in a sealed tube. The reaction solution was cooled with ice, water was added, and extracted with chloroform. The organic layer was washed with water, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (Moritex, acetone:hexane=1:2) to obtain 6-{[2-(2,2-diethoxyethoxy)pyrimidin-5-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine (56 mg, yield: 37%) as a pale brown amorphous solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846700B2
出典データセットuspto-grants-2014_09
ORD IDord-d1e59b377485443ca7fa41e9f0b25ca9
出典メモuspto-grants-2014_09