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HRID 28547作成日:2026年10月24日

Potassium Phosphate, Tribasic → 6-(5-Chloro-2-methoxy-phenyl)-N*2*-(4-chloro-phenyl)-pyrimidine-2,4-diamine

https://huagongshe.com/ja/reaction/28547

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium Phosphate, TribasicHCID 62657—
反応物2-(Dicyclohexylphosphino)biphenylHCID 2734216—
反応物5-Chloro-2-methoxyphenylboronic acidHCID 2735751—
反応物6-Chloro-N2-(4-chlorophenyl)pyrimidine-2,4-diamineHCID 86004316—
触媒palladium(II) acetateHCID 167845—
溶媒TolueneHCID 1140—
溶媒Diethyl EtherHCID 3283—
生成物6-(5-Chloro-2-methoxy-phenyl)-N*2*-(4-chloro-phenyl)-pyrimidine-2,4-diamineHCID 1148521630%

反応条件

温度95 °C

反応手順

A mixture of 6-chloro-N*2*-(4-chloro-phenyl)-pyrimidine-2,4-diamine (0.077 g, 0.30 mmol), 5-chloro-2-methoxy-phenyl boronic acid (0.112 g, 0.60 mmol), palladium (II) acetate (0.017 g, 0.075 mmol), 2-(dicyclohexylphosphino)biphenyl (0.105 g, 0.30 mmol) and potassium phosphate (0.254 g, 1.2 mmol) in dry toluene (3.5 ml) was heated at 90-100° C. under an argon atmosphere for 18 hours. After cooling to room temperature, ether (20 ml) was added and the mixture was washed with aqueous sodium hydroxide solution (1.0 M, 10 ml), with saturated aqueous sodium chloride solution (10 ml), and dried over magnesium sulfate. After concentrating under reduced pressure, the residue was purified by flash chromatography on silica gel eluting with ethyl acetate-hexane (1:3) to provide the title compound (0.032 g, 30% yield) as a white powder.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07419984B2
出典データセットuspto-grants-2008_09
ORD IDord-2a8f2e02149a486185b496f807fc8ddf
出典メモuspto-grants-2008_09