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HRID 10528作成日:2026年10月26日

Cesium fluoride → 4-(4-Fluoro-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine

https://huagongshe.com/reaction/10528

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium fluorideHCID 25953—
反応物4-(4-Bromo-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidineHCID 21979972—
溶媒Dimethyl SulfoxideHCID 679—
生成物4-(4-Fluoro-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidineHCID 2197998823.9%

反応条件

温度150 °C

反応手順

A solution of Intermediate 71 (104 mg) in dimethyl sulfoxide (2 ml) was added with cesium fluoride (284 mg, Wako Pure Chemical Industries) and stirred at 150° C. for 8 hours. The reaction mixture was cooled to room temperature and then filtered through Celite. The residue was added with water (20 ml), extracted with ethyl acetate (20 ml) and washed twice with saturated brine (10 ml for each time). The organic layer was dried over anhydrous sodium sulfate, and then the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (n-hexane:ethyl acetate=3:1) to obtain the title compound (21.1 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07094789B2
出典データセットuspto-grants-2006_08
ORD IDord-da4afad36c4f493fbe7676c2dafd28c1
出典メモuspto-grants-2006_08