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HRID 559075作成日:2026年10月26日

Water → 4-Chloro-2-amino-6-[1-(2-trifluoromethylphenyl)-2,2,2-trifluoro-ethoxy]-pyrimidine

https://huagongshe.com/reaction/559075

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Sodium hydrideHCID 24758—
反応物2-Amino-4,6-dichloropyrimidineHCID 65522—
反応物2,2,2-Trifluoro-1-[2-(trifluoromethyl)phenyl]ethan-1-olHCID 61644993—
溶媒TetrahydrofuranHCID 8028—
溶媒Ethyl AcetateHCID 8857—
生成物4-Chloro-2-amino-6-[1-(2-trifluoromethylphenyl)-2,2,2-trifluoro-ethoxy]-pyrimidineHCID 8661429371.8%

反応条件

温度70 °C

反応手順

NaH (80 mg, 60%, 3.0 mmol) was added to a solution of 1-(2-trifluoromethylphenyl)-2,2,2-trifluoro-ethanol (244 mg, 1 mmol) in 10 ml of anhydrous THF. The mixture was stirred for 20 minutes, 2-amino-4,6-dichloro-pyrimidine (164 mg, 1 mmol) was added and then the reaction mixture was heated at 70° C. for 1 hour. After cooling, 5 ml water was added and ethyl acetate (20 ml) was used to extract the product. The organic layer was dried over sodium sulfate. The solvent was removed by rotovap to give 267 mg of 4-chloro-6-[2,2,2-trifluoro-1-(2-trifluoromethylphenyl)-ethoxy]-pyrimidin-2-ylamine, yield 71%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08063057B2
出典データセットuspto-grants-2011_11
ORD IDord-90724040bb2e491b96ef689a85a2c3ef
出典メモuspto-grants-2011_11