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HRID 337734作成日:2026年10月25日

Cesium carbonate → 3-Fluoro-4-{[(1S*,2R*)-2-(1-methyl-1H-pyrazol-5-yl)cyclopentyl]oxy}-N-(1,3-thiazol-2-yl)benzenesulfonamide

https://huagongshe.com/reaction/337734

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2-BromothiazoleHCID 76430—
反応物trans-N,N'-dimethyl-1,2-cyclohexanediamineHCID 2733821—
反応物3-Fluoro-4-{[(1S*,2R*)-2-(1-methyl-1H-pyrazol-5-yl)cyclopentyl]oxy}benzenesulfonamideHCID 89963259—
触媒Copper iodideHCID 83717—
溶媒DimethylformamideHCID 6228—
生成物3-Fluoro-4-{[(1S*,2R*)-2-(1-methyl-1H-pyrazol-5-yl)cyclopentyl]oxy}-N-(1,3-thiazol-2-yl)benzenesulfonamideHCID 8996366386%

反応手順

A solution of the 3-fluoro-4-{[(1S*,2R*)-2-(1-methyl-1H-pyrazol-5-yl)cyclopentyl]oxy}benzenesulfonamide (0.07 g, 0.21 mmol) prepared in Example 16c, 2-bromothiazole (0.07 g, 0.41 mmol), copper iodide (0.01 g, 0.04 mmol), trans-N,N′-dimethylcyclohexane-1,2-diamine (0.01 g, 0.09 mmol) and cesium carbonate (0.20 g, 0.62 mmol) in DMF (2.0 mL) was stirred at 120° C. for 20 hours under the nitrogen atmosphere. After allowing to cool, the reaction solution was vacuum concentrated, and the residue was purified with HPLC to yield the title compound (75 mg, 86%) as a colorless solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08889741B2
出典データセットuspto-grants-2014_11
ORD IDord-aece0d123fa14c5fa4b22a9eede1b510
出典メモuspto-grants-2014_11