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HRID 598896作成日:2026年10月27日

Cesium carbonate → tert-Butyl(S)-1-(4-chlorophenyl)-4-(4-(isoquinolin-6-yl)-1H-pyrazol-1-yl)butan-2-ylcarbamate

https://huagongshe.com/reaction/598896

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物(S)-3-(tert-butoxycarbonylamino)-4-(4-chlorophenyl)butyl methanesulfonateHCID 57950570—
反応物6-(1H-pyrazol-4-yl)isoquinolineHCID 57950612—
溶媒DimethylformamideHCID 6228—
溶媒Sodium BicarbonateHCID 516892—
生成物tert-Butyl(S)-1-(4-chlorophenyl)-4-(4-(isoquinolin-6-yl)-1H-pyrazol-1-yl)butan-2-ylcarbamateHCID 86635700101.4%

反応手順

A mixture of 6-(1H-pyrazol-4-yl)isoquinoline (130 mg, 0.67 mmol), (S)-3-(tert-butoxycarbonylamino)-4-(4-chlorophenyl)butyl methanesulfonate (327 mg, 0.87 mmol) (prepared as shown in Scheme 15), and cesium carbonate (434 mg, 1.33 mmol) in DMF (5 mL) was stirred at room temperature for 24 hours. The mixture was diluted with saturated aqueous NaHCO3 and extracted with DCM (3×). The combined organic layers were dried over Na2SO4, filtered and concentrated. The residue was purified using column chromatography (acetone/hexanes=0-40%) to provide the product as a tan solid (324 mg, 100%). LCMS (API-ES) m/z: 477 (M+H+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07897619B2
出典データセットuspto-grants-2011_03
ORD IDord-71a33c3e008b4353a56d03f48158d2de
出典メモuspto-grants-2011_03