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HRID 379999作成日:2026年10月25日

Sodium Carbonate → (1S,2R)-4-Fluoro-4'-(2-hydroxy-1-methyl-4-pyridin-3-yl-butoxy)biphenyl-3-carbonitrile

https://huagongshe.com/reaction/379999

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5-Bromo-2-fluorobenzonitrileHCID 2724900—
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)-4-Fluoro-4'-(2-hydroxy-1-methyl-4-pyridin-3-yl-butoxy)biphenyl-3-carbonitrileHCID 53853615—

反応条件

温度80 °C

反応手順

Prepared according to the method described in Example 12 from (1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid (0.4 g, Example 33), 3-cyano-4-flurobromobenzene (0.399 g), ethanol (10 ml), 2M aqueous sodium carbonate (1.66 ml) and tetrakis(triphenylphosphine)palladium (0) (0.3 g) with heating at 80° C. for 3 hours. After work-up, the residue was purified by normal-phase HPLC eluting a gradient of 0-10% ethanol in dichloromethane to give the title compound as a solid. (0.24 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-57fa8a56fc5f40a5ba86f6c4c8cea0aa
出典メモuspto-grants-2001_10