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HRID 380002作成日:2026年10月25日

Sodium Carbonate → (1S,2R)-3-Chloro-4'-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)biphenyl-4-carbonitrile

https://huagongshe.com/reaction/380002

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物4-Bromo-2-chlorobenzonitrileHCID 7010420—
反応物(1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acidHCID 54413593—
触媒HCID 178418397HCID 178418397—
溶媒EthanolHCID 702—
生成物(1S,2R)-3-Chloro-4'-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)biphenyl-4-carbonitrileHCID 5719177269%

反応条件

温度90 °C

反応手順

Prepared according to the method described in Example 12b) from (1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid (0.20 g, Example 33), 4-bromo-2-chlorobenzonitrile (0.288 g), 2M aqueous sodium carbonate (0.76 ml) and tetrakis(triphenylphosphine)palladium (0) (0.075 g) in ethanol (5 ml) with heating at 90° C. for 4 hours. After work up, the residue was purified by normal-phase HPLC eluting with a gradient of 0-10% ethanol in dichloromethane to give the title compound as an oil (0.18 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06300352B1
出典データセットuspto-grants-2001_10
ORD IDord-1e795bac0e8943e7ad5ad9d9ee0d679e
出典メモuspto-grants-2001_10