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HRID 81625作成日:2026年10月26日

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

https://huagongshe.com/reaction/81625

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5-(2,2-Diethoxyethoxy)-2-fluoropyridineHCID 68429706—
溶媒WaterHCID 962—
生成物6-{[5-(2,2-diethoxyethoxy)pyridin-2-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amineHCID 6842977565%

反応条件

温度170 °C

反応手順

5-(2,2-diethoxyethoxy)-2-fluoropyridine (502 mg, 2.19 mmol) and potassium tert-butoxide (279 mg, 2.49 mmol) were added to an N,N-dimethylacetamide solution (1 ml) of 4-[(1-methyl-1H-pyrazol-3-yl)amino]quinazolin-6-ol (240 mg, 1.00 mmol), and stirred at 170° C. for 15 hours under a nitrogen atmosphere in a sealed tube. The reaction solution was cooled to room temperature, then 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 (Biotage, chloroform:methanol=100:3) to obtain 6-{[5-(2,2-diethoxyethoxy)pyridin-2-yl]oxy}-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine (292 mg, yield: 65%) as a brown oil.

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-c6d2e65ddbf94c72b551a36e2c02a94f
出典メモuspto-grants-2014_09