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HRID 2391362作成日:2026年10月26日

Water → N-[5-({2-[(cyclopropylsulfonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-fluorophenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide

https://huagongshe.com/reaction/2391362

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物TriethylamineHCID 8471—
反応物Cyclopropanesulfonyl chlorideHCID 2760919—
反応物N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-fluorophenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide hydrochlorideHCID 57505567—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物N-[5-({2-[(cyclopropylsulfonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-fluorophenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamideHCID 5750560116%

反応条件

温度70 °C

反応手順

To a solution of N-{5-[(2-aminoimidazo[1,2-b]pyridazin-6-yl)oxy]-2-fluorophenyl}-1,3-dimethyl-1H-pyrazole-5-carboxamide.hydrochloride (400 mg, 0.97 mmol) in 1-methyl-2-pyrrolidone (4.0 mL) were added triethylamine (404 μL, 2.90 mmol) and cyclopropanesulfonyl chloride (204 mg, 1.45 mmol), and the mixture was stirred at 70° C. for 16 hr. After cooling the mixture to room temperature, water was added to the reaction mixture, and the mixture was extracted with ethyl acetate/tetrahydrofuran, washed with saturated brine, dried over anhydrous sodium sulfate, and filtrated. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate alone) and precipitated from hexane/ethyl acetate to give the title compound (74 mg, 16%) as a white powder.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08273741B2
出典データセットuspto-grants-2012_09
ORD IDord-0cfc9906225241b0a8c8012d79d439f5
出典メモuspto-grants-2012_09