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HRID 1520268作成日:2026年10月26日

1,2-Dimethoxyethane → 4-((1-(4-(5-Chloropyrimidin-2-yl)-2-methylphenyl)-4,4,4-trifluorobutyl)amino)benzoic acid

https://huagongshe.com/reaction/1520268

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DimethoxyethaneHCID 8071—
反応物Sodium CarbonateHCID 10340—
反応物2-Bromo-5-chloropyrimidineHCID 22236273—
反応物4-((4,4,4-Trifluoro-1-(2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)butyl)amino)benzoic acidHCID 131733104—
触媒HCID 178418397HCID 178418397—
溶媒WaterHCID 962—
生成物4-((1-(4-(5-Chloropyrimidin-2-yl)-2-methylphenyl)-4,4,4-trifluorobutyl)amino)benzoic acidHCID 11784035183.8%

反応条件

温度130 °C

反応手順

A reaction mixture of 4-((4,4,4-trifluoro-1-(2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)butyl)amino)benzoic acid (0.500 g), 2-bromo-5-chloropyrimidine (0.251 g), tetrakistriphenylphosphinepalladium (0.125 g), sodium carbonate (0.343 g), DME (3 mL) and water (1 mL) was stirred at 130° C. for 1 hr under microwave irradiation under a nitrogen atmosphere. The reaction mixture was added to water, and the mixture was extracted with ethyl acetate. The extract was washed with water and saturated brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure and the residue was purified by silica gel column chromatography (hexane/ethyl acetate) to give the title compound (0.407 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09073864B2
出典データセットuspto-grants-2015_07
ORD IDord-fadce8056bb14423aa1724b93c26f1cb
出典メモuspto-grants-2015_07